PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 26005563-6 2015 Modeling of compound 10 in the active site of HDAC2 demonstrates that the 2-(oxazol-2-yl)phenol moiety has a zinc-binding pattern similar to benzamide HDAC inhibitors. benzamide 141-150 histone deacetylase 2 Homo sapiens 46-51 25893048-0 2015 Novel benzamide-based histamine h3 receptor antagonists: the identification of two candidates for clinical development. benzamide 6-15 histamine receptor H3 Homo sapiens 22-43 25515955-0 2015 Design, synthesis and structure-activity relationship studies of novel sirtuin 2 (SIRT2) inhibitors with a benzamide skeleton. benzamide 107-116 sirtuin 2 Homo sapiens 71-80 25402753-8 2015 Structure-function studies determined that disruption of Hsp90alpha/Aha1 association and inhibition of cell migration correlated with the presence of a benzamide side chain, since an acetamide substituted analog was less effective. benzamide 152-161 heat shock protein 90 alpha family class A member 1 Homo sapiens 57-67 25402753-8 2015 Structure-function studies determined that disruption of Hsp90alpha/Aha1 association and inhibition of cell migration correlated with the presence of a benzamide side chain, since an acetamide substituted analog was less effective. benzamide 152-161 activator of HSP90 ATPase activity 1 Homo sapiens 68-72 25515955-0 2015 Design, synthesis and structure-activity relationship studies of novel sirtuin 2 (SIRT2) inhibitors with a benzamide skeleton. benzamide 107-116 sirtuin 2 Homo sapiens 82-87 25515955-2 2015 We designed and synthesized a series of benzamide derivatives as SIRT2 inhibitor candidates. benzamide 40-49 sirtuin 2 Homo sapiens 65-70 26282548-4 2015 Chidamide, a novel benzamide-type selectively HDAC inhibitor, has been reported to induce G1 arrest and apoptosis in the relatively mature progenitor population, whereas its effect on primitive LSCs has not been clarified. benzamide 19-28 histone deacetylase 9 Homo sapiens 46-50 25115329-0 2014 Phenyl amide linker improves the pharmacokinetics and pharmacodynamics of N-terminally mono-PEGylated human growth hormone. benzamide 0-12 growth hormone 1 Homo sapiens 108-122 25262942-3 2014 In this study, we further explored SAR through a combination of traditional medicinal chemistry and structure-based drug design, resulting in a novel scaffold (benzamide) with selectivity against protein kinases. benzamide 160-169 sarcosine dehydrogenase Homo sapiens 35-38 25360823-4 2014 For HDAC1/2/3 selective-inhibitor benzamide, the conserved tyrosine could modulate the coordinative ability of the central atom (Zn(2+)), while for pan-inhibitor SAHA, the conserved tyrosine could increase the chelating ability of the ligand (SAHA). benzamide 34-43 histone deacetylase 1 Homo sapiens 4-13 24559867-4 2014 The phenyl amide disila compound 22 showed the most potent ROR-inhibitory activity among the compounds examined. benzamide 4-16 long intergenic non-protein coding RNA, regulator of reprogramming Homo sapiens 59-62 24721323-2 2014 Chidamide is a novel benzamide chemical class of HDAC inhibitor that selectively inhibited HDAC1, 2, 3 and 10. benzamide 21-30 histone deacetylase 1 Homo sapiens 91-109 24638994-4 2014 In human ether-a-go-go-related gene 1 (hERG1) K(+) channels, C-type inactivation is allosterically inhibited by ICA-105574, a substituted benzamide. benzamide 138-147 potassium voltage-gated channel subfamily H member 2 Homo sapiens 39-44 24878359-9 2014 These findings strongly support our assumption that the fragment of benzamide can replace the pyridine ring in some PI3K and mTOR dual inhibitor to design novel anticancer agents. benzamide 68-77 mechanistic target of rapamycin kinase Homo sapiens 125-129 24789078-2 2014 Removal of the benzamide group of the intermediates could furnish chiral C-1 substituted tetrahydroisoquinolines (see scheme) in high yields and excellent stereoselectivities. benzamide 15-24 heterogeneous nuclear ribonucleoprotein C Homo sapiens 73-76 24900823-0 2014 Phenyl carboxamide analogues as spleen tyrosine kinase (syk) inhibitors. benzamide 0-18 spleen associated tyrosine kinase Homo sapiens 56-59 24881658-1 2014 Synthesis and structure-activity relationship of a novel series of isoquinoline CRTH2 antagonists bearing a methylene linker between the isoquinoline and benzamide moieties were described. benzamide 154-163 prostaglandin D2 receptor 2 Cavia porcellus 80-85 24405209-9 2014 The intermediacy of an alkyl radical was evidenced by the catalytic reaction of cyclohexane with benzamide in the presence of CBr4, which formed exclusively bromocyclohexane. benzamide 97-106 carbonyl reductase 4 Homo sapiens 126-130 23757208-2 2013 We exploited knowledge on nAChR ligands and their binding site that were previously identified by our laboratory through virtual screenings and identified benzamide analogs as a novel chemical class of neuronal nicotinic receptor (nAChR) ligands. benzamide 155-164 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 26-31 25450624-3 2014 In vitro enzymatic assay at 10 microM against all the eight human PI3K isoforms showed that an unsubstituted benzamide group at position 6 and an acetyl group at N(4) gave the best inhibitory activity on PI3Kgamma. benzamide 109-118 phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma Homo sapiens 204-213 25254219-2 2014 A 18F-labeled benzamide derivative, [18F]N-(2-diethylaminoethyl)-4-[2-(2-(2-fluoroethoxy) ethoxy)ethoxy]benzamide ([18F]FPBZA), was developed as a promising PET probe for primary and metastatic melanoma. benzamide 14-23 thyroid stimulating hormone receptor Mus musculus 157-160 24256509-2 2013 Arylation was accomplished using either Ni(COD)2 or 1,10-phenanthroline in substoichiometric amounts, and the reaction conditions were applied to a variety of electronically differentiated benzamide substrates. benzamide 189-198 COD2 Homo sapiens 43-48 23757208-2 2013 We exploited knowledge on nAChR ligands and their binding site that were previously identified by our laboratory through virtual screenings and identified benzamide analogs as a novel chemical class of neuronal nicotinic receptor (nAChR) ligands. benzamide 155-164 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 231-236 23333209-1 2013 AX10479, the phenyl amide of 4-hydroxy-8-methanesulfonylamino-quinoline-2-carboxylic acid, was identified as a Zn(2+)-dependent, 27nM inhibitor of human plasma Lp-PLA(2). benzamide 13-25 phospholipase A2 group VII Homo sapiens 160-168 23652817-3 2013 Using suitable proxies arranged in pseudo-crystalline setups we discriminate the contribution of hydrogen bonding, pi-pi interactions and intra-molecular interactions to the lattice energies of the most relevant (P1 and P3) benzamide polymorphs. benzamide 224-233 crystallin gamma F, pseudogene Homo sapiens 213-222 23656327-4 2013 Specifically, a subset of compounds bearing phenyl and substituted phenyl carboxamides induced lower IL-6 release while maintaining higher IP-10 production, skewing toward the type I interferon pathway. benzamide 67-86 interleukin 6 Homo sapiens 101-105 23656327-4 2013 Specifically, a subset of compounds bearing phenyl and substituted phenyl carboxamides induced lower IL-6 release while maintaining higher IP-10 production, skewing toward the type I interferon pathway. benzamide 67-86 C-X-C motif chemokine ligand 10 Homo sapiens 139-144 23218712-1 2013 Novel benzamide derivatives were synthesized and tested at in vitro assay by measuring fold increase of glucokinase activity at 5.0 mM glucose concentration. benzamide 6-15 glucokinase Mus musculus 104-115 23380375-2 2013 Optimization of the benzamide and central ring components of the core scaffold led to the identification of a GlyT-1 inhibitor that demonstrated in vivo activity in a rodent cerebral spinal fluid (CSF) glycine model. benzamide 20-29 solute carrier family 6 member 9 Homo sapiens 110-116 22588261-0 2012 Ring substituents on substituted benzamide ligands indirectly mediate interactions with position 7.39 of transmembrane helix 7 of the D4 dopamine receptor. benzamide 33-42 dopamine receptor D4 Homo sapiens 134-154 23042668-2 2012 Here, lead optimization of H(3)R inverse agonists bearing a thiazolo[5,4-c]piperidine group gave rise to a clinical candidate with a much simpler unprecedented benzamide scaffold, displaying decreased hERG activity while maintaining high brain receptor occupancies. benzamide 160-169 ETS transcription factor ERG Homo sapiens 201-205 22818799-0 2012 Induction of differentiation and apoptosis in leukaemic cell lines by the novel benzamide family histone deacetylase 2 and 3 inhibitor MI-192. benzamide 80-89 histone deacetylase 2 Homo sapiens 97-124 22818799-3 2012 More complex second generation HDACIs undergoing clinical trials, such as the benzamide group compounds MS-275 and MGCD0103, are specific primarily for HDAC1 and HDAC2. benzamide 78-87 histone deacetylase 1 Homo sapiens 152-157 22818799-3 2012 More complex second generation HDACIs undergoing clinical trials, such as the benzamide group compounds MS-275 and MGCD0103, are specific primarily for HDAC1 and HDAC2. benzamide 78-87 histone deacetylase 2 Homo sapiens 162-167 23123015-0 2012 Design, synthesis, and evaluation of imidazo[1,2-b]pyridazine derivatives having a benzamide unit as novel VEGFR2 kinase inhibitors. benzamide 83-92 kinase insert domain receptor Homo sapiens 107-113 23263798-3 2012 Novel benzamide derivatives were synthesized and tested using in vitro assays by measuring fold increase of glucokinase activity at 5.0 mM glucose concentration. benzamide 6-15 glucokinase Mus musculus 108-119 22939233-0 2012 Benzimidazoles as benzamide replacements within cyclohexane-based CC chemokine receptor 2 (CCR2) antagonists. benzamide 18-27 C-C motif chemokine receptor 2 Homo sapiens 66-89 22939233-0 2012 Benzimidazoles as benzamide replacements within cyclohexane-based CC chemokine receptor 2 (CCR2) antagonists. benzamide 18-27 C-C motif chemokine receptor 2 Homo sapiens 91-95 22771007-0 2012 Design, synthesis, modeling, biological evaluation and photoaffinity labeling studies of novel series of photoreactive benzamide probes for histone deacetylase 2. benzamide 119-128 histone deacetylase 2 Homo sapiens 140-161 22459213-1 2012 A series of benzamide derivatives were assembled by using the privileged-fragment-merging (PFM) strategy and their SAR studies as glucokinase activators were described. benzamide 12-21 sarcosinemia autosomal recessive Mus musculus 115-118 22396044-0 2012 A benzamide-linked small molecule NDMC101 inhibits NFATc1 and NF-kappaB activity: a potential osteoclastogenesis inhibitor for experimental arthritis. benzamide 2-11 nuclear factor of activated T cells, cytoplasmic, calcineurin dependent 1 Mus musculus 51-57 22396044-0 2012 A benzamide-linked small molecule NDMC101 inhibits NFATc1 and NF-kappaB activity: a potential osteoclastogenesis inhibitor for experimental arthritis. benzamide 2-11 nuclear factor of kappa light polypeptide gene enhancer in B cells 1, p105 Mus musculus 62-71 22217870-1 2012 AX10185, the phenyl amide of xanthurenic acid, was found to be a sub-100nM inhibitor of Lp-PLA(2). benzamide 13-25 phospholipase A2 group VII Homo sapiens 88-96 22277094-3 2012 Benzoyl 6 and benzamide 17 are the most selective compounds toward 17beta-HSD2 described so far. benzamide 14-23 hydroxysteroid 17-beta dehydrogenase 2 Homo sapiens 67-78 21507637-1 2011 Seeking compounds preferentially potent and selective for MMP-13, we reported in the preceding Letter on a series of hydroxamic acids with a flexible benzamide tail groups. benzamide 150-159 matrix metallopeptidase 13 Rattus norvegicus 58-64 21858617-0 2011 A benzamide-linked small molecule HS-Cf inhibits TNF-alpha-induced interferon regulatory factor-1 in porcine chondrocytes: a potential disease-modifying drug for osteoarthritis therapeutics. benzamide 2-11 tumor necrosis factor Sus scrofa 49-58 21858617-0 2011 A benzamide-linked small molecule HS-Cf inhibits TNF-alpha-induced interferon regulatory factor-1 in porcine chondrocytes: a potential disease-modifying drug for osteoarthritis therapeutics. benzamide 2-11 interferon regulatory factor 1 Sus scrofa 67-97 21858617-8 2011 RESULTS: Bioassay screening of benzamide-linked small molecules revealed that 2-hydroxy-N-[3-(trifluoromethyl)phenyl]benzamide (HS-Cf) was a potent inhibitor of NO production and iNOS expression in TNF-alpha-stimulated porcine chondrocytes. benzamide 31-40 LOC396821 Sus scrofa 179-183 21858617-8 2011 RESULTS: Bioassay screening of benzamide-linked small molecules revealed that 2-hydroxy-N-[3-(trifluoromethyl)phenyl]benzamide (HS-Cf) was a potent inhibitor of NO production and iNOS expression in TNF-alpha-stimulated porcine chondrocytes. benzamide 31-40 tumor necrosis factor Sus scrofa 198-207 21858617-13 2011 CONCLUSIONS: In a minilibrary containing 300 small molecules, we identified a benzamide-linked small molecule, HS-Cf, that through down-regulating TNF-alpha-induced IRF-1 activity suppressed chondrocyte activation and prevented cartilage destruction. benzamide 78-87 tumor necrosis factor Sus scrofa 147-156 21858617-13 2011 CONCLUSIONS: In a minilibrary containing 300 small molecules, we identified a benzamide-linked small molecule, HS-Cf, that through down-regulating TNF-alpha-induced IRF-1 activity suppressed chondrocyte activation and prevented cartilage destruction. benzamide 78-87 interferon regulatory factor 1 Sus scrofa 165-170 21782424-1 2011 A non-estrogenic inhibitor of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) was designed based on a modified 3-hydroxy-estra-1,3,5(10)-triene core having an additional five-member lactone ring and a benzamide group. benzamide 210-219 RNA, U1 small nuclear 1 Homo sapiens 6-85 21414780-4 2011 Increasing the acidity of the amide proton by converting the benzamide in lead 1 to an anilide provided single digit nanomolar MCHR1 antagonists while replacing the dimethoxyphenyl ring of 1 with alkyl groups possessing increased polarity dramatically reduced the hERG inhibition. benzamide 61-70 melanin concentrating hormone receptor 1 Homo sapiens 127-132 21246737-2 2011 The design, synthesis, and functional characterisation of benzamide analogues at the 5-HT3A receptor yielded substantial information concerning the analogues as 5-HT3 receptor agonists. benzamide 58-67 5-hydroxytryptamine receptor 3A Homo sapiens 85-91 21316218-2 2011 Design and synthesis of a novel MEK inhibitor, based on the 3D-structural information of the target enzyme, and then multidimensional optimization including metabolic stability, physicochemical properties and safety profiles were effectively performed and led to the identification of a clinical candidate for an orally available potent MEK inhibitor, CH4987655, possessing a unique 3-oxo-oxazinane ring structure at the 5-position of the benzamide core structure. benzamide 439-448 mitogen-activated protein kinase kinase 7 Homo sapiens 32-35 21316218-2 2011 Design and synthesis of a novel MEK inhibitor, based on the 3D-structural information of the target enzyme, and then multidimensional optimization including metabolic stability, physicochemical properties and safety profiles were effectively performed and led to the identification of a clinical candidate for an orally available potent MEK inhibitor, CH4987655, possessing a unique 3-oxo-oxazinane ring structure at the 5-position of the benzamide core structure. benzamide 439-448 mitogen-activated protein kinase kinase 7 Homo sapiens 337-340 21904660-1 2010 Structural modifications to the coumarin core and benzamide side chain of novobiocin have successfully transformed the natural product from a selective DNA gyrase inhibitor into a potent inhibitor of the Hsp90 C-terminus. benzamide 50-59 heat shock protein 90 alpha family class A member 1 Homo sapiens 204-209 20709754-10 2010 Flecainide docking in the Kv1.2-based homology model of Kv2.1 predicts the ligand ammonium group in the central cavity and the benzamide moiety in a niche between S6 and the P-helix. benzamide 127-136 potassium channel, voltage gated shaker related subfamily A, member 2 L homeolog Xenopus laevis 26-31 20709754-10 2010 Flecainide docking in the Kv1.2-based homology model of Kv2.1 predicts the ligand ammonium group in the central cavity and the benzamide moiety in a niche between S6 and the P-helix. benzamide 127-136 potassium channel, voltage gated Shab related subfamily B, member 1 S homeolog Xenopus laevis 56-61 20705631-3 2010 We aimed to evaluate the efficacy of benzamide, a PARP inhibitor, in an experimental model of ANP. benzamide 37-46 poly (ADP-ribose) polymerase 1 Rattus norvegicus 50-54 20705631-13 2010 We observed that inhibition of PARP with benzamide reduced the severity, the mortality, the bacterial translocation rates and the neopterin concentrations in an experimental ANP model in rats. benzamide 41-50 poly (ADP-ribose) polymerase 1 Rattus norvegicus 31-35 20045315-1 2010 Through conformational restriction of a benzamide by formation of a seven-membered hydrogen-bond with an oxindole carbonyl group, a series of PARP inhibitors was designed for appropriate orientation for binding to the PARP surface. benzamide 40-49 poly(ADP-ribose) polymerase 1 Homo sapiens 142-146 19998477-2 2010 Here we investigated the therapeutic effect of the PARP inhibitor benzamide against 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) neurotoxicity in mice. benzamide 66-75 poly (ADP-ribose) polymerase family, member 1 Mus musculus 51-55 19998477-5 2010 Furthermore, our immunohistochemical study showed that posttreatment with benzamide significantly prevented neuronal damage by suppressing overexpression of neuronal, microglial, and astroglial PARP after MPTP treatment. benzamide 74-83 poly (ADP-ribose) polymerase family, member 1 Mus musculus 194-198 20045315-1 2010 Through conformational restriction of a benzamide by formation of a seven-membered hydrogen-bond with an oxindole carbonyl group, a series of PARP inhibitors was designed for appropriate orientation for binding to the PARP surface. benzamide 40-49 poly(ADP-ribose) polymerase 1 Homo sapiens 218-222 19758809-0 2009 Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase. benzamide 0-9 glucokinase Homo sapiens 106-117 19811913-2 2009 Thus, extending the length of the original benzamide side chain by a single methylene unit imparts CCK1R affinity to the series, and further fine tuning of the affinity results in CCK1R selectivity of greater than 100-fold. benzamide 43-52 cholecystokinin A receptor Homo sapiens 99-104 19811913-2 2009 Thus, extending the length of the original benzamide side chain by a single methylene unit imparts CCK1R affinity to the series, and further fine tuning of the affinity results in CCK1R selectivity of greater than 100-fold. benzamide 43-52 cholecystokinin A receptor Homo sapiens 180-185 20181479-0 2010 Heterocyclic acetamide and benzamide derivatives as potent and selective beta3-adrenergic receptor agonists with improved rodent pharmacokinetic profiles. benzamide 27-36 adrenoceptor beta 3 Homo sapiens 73-98 20641656-15 2004 Most benzamide derivatives possess the common structure element of Ph-CONH(CH2)mNR2 (m = 1,2), and they exhibit comparable properties such as high melanoma uptake, which is a positive attribute for potentially useful imaging agents (11). benzamide 5-14 motor neuron and pancreas homeobox 1 Mus musculus 79-83 20641666-15 2004 Most benzamide derivatives possess the common structure element of Ph-CONH(CH2)mNR2 (m = 1,2), and they exhibit comparable properties such as high melanoma uptake, which is a positive attribute for potentially useful imaging agents (12). benzamide 5-14 motor neuron and pancreas homeobox 1 Mus musculus 79-83 19758809-1 2009 A series of benzamide derivatives which can simultaneously inhibit glycogen phosphorylase (GP) and activate glucokinase (GK) were prepared and evaluated. benzamide 12-21 glucokinase Homo sapiens 108-119 19758809-1 2009 A series of benzamide derivatives which can simultaneously inhibit glycogen phosphorylase (GP) and activate glucokinase (GK) were prepared and evaluated. benzamide 12-21 glucokinase Homo sapiens 121-123 19664921-4 2009 The piperazine ring was shown to be a critical element of the HIV-1 attachment inhibiting pharmacophore, acting as a scaffold to deploy the indole glyoxamide and benzamide in a topographical relationship that complements the binding site on gp120. benzamide 162-171 Envelope surface glycoprotein gp160, precursor Human immunodeficiency virus 1 241-246 19447888-6 2009 Furthermore, PARP-1 inhibitor (benzamide) decreased PARP-1 binding to G(-172) --> T without affecting mRNA or protein expression level of PARP-1 and down-regulated the subsequent MOR gene expression in SH-SY5Y cells. benzamide 31-40 poly(ADP-ribose) polymerase 1 Homo sapiens 13-19 19447888-6 2009 Furthermore, PARP-1 inhibitor (benzamide) decreased PARP-1 binding to G(-172) --> T without affecting mRNA or protein expression level of PARP-1 and down-regulated the subsequent MOR gene expression in SH-SY5Y cells. benzamide 31-40 poly(ADP-ribose) polymerase 1 Homo sapiens 52-58 19447888-6 2009 Furthermore, PARP-1 inhibitor (benzamide) decreased PARP-1 binding to G(-172) --> T without affecting mRNA or protein expression level of PARP-1 and down-regulated the subsequent MOR gene expression in SH-SY5Y cells. benzamide 31-40 poly(ADP-ribose) polymerase 1 Homo sapiens 52-58 19447888-6 2009 Furthermore, PARP-1 inhibitor (benzamide) decreased PARP-1 binding to G(-172) --> T without affecting mRNA or protein expression level of PARP-1 and down-regulated the subsequent MOR gene expression in SH-SY5Y cells. benzamide 31-40 opioid receptor mu 1 Homo sapiens 179-182 19200741-6 2009 We will present the synthesis, biological activities and SAR study of a series of pyrazolo[1,5-a]pyrimidines with an optimized phenyl amide moiety at the C-7 position. benzamide 127-139 sarcosine dehydrogenase Homo sapiens 57-60 19350613-1 2009 We compare three structurally different classes of histone deacetylase (HDAC) inhibitors that contain benzamide, hydroxamate, or thiol groups as the zinc binding group (ZBG) for their ability to protect cortical neurons in culture from cell death induced by oxidative stress. benzamide 102-111 histone deacetylase 9 Homo sapiens 51-70 19350613-1 2009 We compare three structurally different classes of histone deacetylase (HDAC) inhibitors that contain benzamide, hydroxamate, or thiol groups as the zinc binding group (ZBG) for their ability to protect cortical neurons in culture from cell death induced by oxidative stress. benzamide 102-111 histone deacetylase 9 Homo sapiens 72-76 19246196-1 2009 Benzamide 1 demonstrated good potency as a selective ITK inhibitor, however the amide moiety was found to be hydrolytically labile in vivo, resulting in low oral exposure and the generation of mutagenic aromatic amine metabolites. benzamide 0-9 IL2 inducible T cell kinase Homo sapiens 53-56 18155908-0 2008 Synthesis of benzamide derivatives as TRPV1 antagonists. benzamide 13-22 transient receptor potential cation channel subfamily V member 1 Homo sapiens 38-43 18501976-1 2008 The present study is aimed at evaluating the functional and neuroprotective effect of benzamide, a poly-(ADP-ribose) polymerase (PARP) inhibitor on delayed neuronal death (DND) in hippocampus CA1 region and memory impairment following global cerebral ischemia (GCI) in a mouse model. benzamide 86-95 poly (ADP-ribose) polymerase family, member 1 Mus musculus 99-127 18501976-1 2008 The present study is aimed at evaluating the functional and neuroprotective effect of benzamide, a poly-(ADP-ribose) polymerase (PARP) inhibitor on delayed neuronal death (DND) in hippocampus CA1 region and memory impairment following global cerebral ischemia (GCI) in a mouse model. benzamide 86-95 poly (ADP-ribose) polymerase family, member 1 Mus musculus 129-133 18501976-1 2008 The present study is aimed at evaluating the functional and neuroprotective effect of benzamide, a poly-(ADP-ribose) polymerase (PARP) inhibitor on delayed neuronal death (DND) in hippocampus CA1 region and memory impairment following global cerebral ischemia (GCI) in a mouse model. benzamide 86-95 carbonic anhydrase 1 Mus musculus 192-195 18501976-6 2008 It is clear from the present experiment that benzamide treatment significantly decreases the iNOS expression and number of apoptotic neurons and thereby improves the neuronal survival and memory during GCI. benzamide 45-54 nitric oxide synthase 2, inducible Mus musculus 93-97 18553955-0 2008 Discovery of novel, potent benzamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) exhibiting oral activity in an enzyme inhibition ex vivo model. benzamide 27-36 RNA, U1 small nuclear 1 Homo sapiens 51-106 18553955-1 2008 We report the discovery of potent benzamide inhibitors of 11beta-hydroxysteroid dehydrogenase (11beta-HSD1). benzamide 34-43 hydroxysteroid 11-beta dehydrogenase 1 Homo sapiens 95-106 18695944-2 2009 Benzamide (BA) and 4-amino-1,8-naphthalimide (NAP), two well-known inhibitors of PARP, treatment increased nuclear fragmentation and caspase-3 activity in HeLa (Human cervical cancer cell line) cells. benzamide 0-9 poly(ADP-ribose) polymerase 1 Homo sapiens 81-85 18695944-2 2009 Benzamide (BA) and 4-amino-1,8-naphthalimide (NAP), two well-known inhibitors of PARP, treatment increased nuclear fragmentation and caspase-3 activity in HeLa (Human cervical cancer cell line) cells. benzamide 0-9 caspase 3 Homo sapiens 133-142 18695944-2 2009 Benzamide (BA) and 4-amino-1,8-naphthalimide (NAP), two well-known inhibitors of PARP, treatment increased nuclear fragmentation and caspase-3 activity in HeLa (Human cervical cancer cell line) cells. benzamide 11-13 poly(ADP-ribose) polymerase 1 Homo sapiens 81-85 18695944-2 2009 Benzamide (BA) and 4-amino-1,8-naphthalimide (NAP), two well-known inhibitors of PARP, treatment increased nuclear fragmentation and caspase-3 activity in HeLa (Human cervical cancer cell line) cells. benzamide 11-13 caspase 3 Homo sapiens 133-142 18695944-5 2009 PARP-1 knock down cells were sensitive to BA induced nuclear fragmentation and caspase-3 activation while exogenous expression of PARP-1 rendered cells resistant to BA induced apoptosis. benzamide 42-44 poly(ADP-ribose) polymerase 1 Homo sapiens 0-6 18695944-5 2009 PARP-1 knock down cells were sensitive to BA induced nuclear fragmentation and caspase-3 activation while exogenous expression of PARP-1 rendered cells resistant to BA induced apoptosis. benzamide 165-167 poly(ADP-ribose) polymerase 1 Homo sapiens 130-136 18599297-1 2008 In the investigation of the structure-activity relationship of nonpeptide AT(2) receptor agonists, a series of substituted benzamide analogues of the selective nonpeptide AT(2) receptor agonist M024 have been synthesised. benzamide 123-132 angiotensin II receptor, type 2 Mus musculus 171-185 18155908-2 2008 Compound 1 has led to potent TRPV1 antagonistic benzamide derivatives ((+/-)-2: human IC(50)=23 nM, (+/-)-3: human IC(50)=14 nM in the capsaicin-induced calcium influx assay) containing indole and naphthyl moieties, obtained by elaboration of the tryptamine scaffold or via bioisosteric replacements. benzamide 48-57 transient receptor potential cation channel subfamily V member 1 Homo sapiens 29-34 18673170-0 2008 Histone deacetylase inhibitors in cancer therapy: new compounds and clinical update of benzamide-type agents. benzamide 87-96 histone deacetylase 9 Homo sapiens 0-19 17951061-4 2008 Further structural modifications of the benzamide and piperidine moieties of 1 led to the identification of exo-N-{8-[(6-fluoro-2-naphthyl)methyl]-8-azabicyclo[3.2.1]oct-3- yl}biphenyl-2-carboxamide [corrected] (31) as a potent CCR3 antagonist with an IC(50) value of 0.020 microM. benzamide 40-49 C-C motif chemokine receptor 3 Homo sapiens 228-232 18850361-1 2008 S-3-iodo-N-(1-ethyl-2-pyrrolidinyl)methyl-2-hydroxy-6-methoxybenzamide (IBZM) is one of the several benzamide derivatives showing a high affinity for the central nervous system (CNS) D2 dopamine receptor. benzamide 61-70 dopamine receptor D2 Rattus norvegicus 183-203 17210149-1 2007 The 1:1 inclusion complex of beta-cyclodextrin and benzamide was prepared and characterized by single crystal X-ray diffraction, PXRD, TGA, and IR. benzamide 51-60 T-box transcription factor 1 Homo sapiens 135-138 17896912-4 2007 Since the early benzamide inhibitors of the 1980s PARP inhibitors, developed through structure-activity relationships and crystal structure-based drug design, that are 1,000 x more potent have been identified. benzamide 16-25 poly(ADP-ribose) polymerase 1 Homo sapiens 50-54 17455259-0 2007 Distinct pharmacological properties of second generation HDAC inhibitors with the benzamide or hydroxamate head group. benzamide 82-91 histone deacetylase 9 Homo sapiens 57-61 17728843-8 2007 These changes were prevented by the PARP inhibitors benzamide or DPQ (3,4-dihydro-5-[4-(1-piperidinyl)butoxyl]-1(2H)-isoquinolinone) or PARP-1 gene deletion (PARP-1 KO). benzamide 52-61 poly(ADP-ribose) polymerase 1 Homo sapiens 36-40 17728843-8 2007 These changes were prevented by the PARP inhibitors benzamide or DPQ (3,4-dihydro-5-[4-(1-piperidinyl)butoxyl]-1(2H)-isoquinolinone) or PARP-1 gene deletion (PARP-1 KO). benzamide 52-61 poly(ADP-ribose) polymerase 1 Homo sapiens 136-142 17728843-8 2007 These changes were prevented by the PARP inhibitors benzamide or DPQ (3,4-dihydro-5-[4-(1-piperidinyl)butoxyl]-1(2H)-isoquinolinone) or PARP-1 gene deletion (PARP-1 KO). benzamide 52-61 poly(ADP-ribose) polymerase 1 Homo sapiens 158-164 16724231-0 2006 The benzamide M344, a novel histone deacetylase inhibitor, significantly increases SMN2 RNA/protein levels in spinal muscular atrophy cells. benzamide 4-13 survival of motor neuron 2, centromeric Homo sapiens 83-87 17169559-5 2007 Furthermore, SAR analysis suggests that steric, electronic, and lipophilic characteristics of substituents in the benzamide region of DNK333 have a crucial effect on both the NK(1) and NK(2) receptor antagonist activities. benzamide 114-123 tachykinin receptor 2 Homo sapiens 185-199 16288681-4 2006 In this study, we measured dopamine D2 receptor occupancy of two conventional benzamide antipsychotics, sulpiride and sultopride, using positron emission tomography, to investigate the rationale of their clinical dose. benzamide 78-87 dopamine receptor D2 Homo sapiens 27-47 16724231-6 2006 Here we show that the novel benzamide M344, an HDAC inhibitor, up-regulates SMN2 protein expression in fibroblast cells derived from SMA patients up to 7-fold after 64 h of treatment. benzamide 28-37 survival of motor neuron 2, centromeric Homo sapiens 76-80 17249247-0 2006 The benzamide derivative N-[1-(7-tert-Butyl-1H-indol-3-ylmethyl)-2-(4-cyclopropanecarbonyl-3-methyl-piperazin-1-yl)-2-oxo-ethyl]-4-nitro-benzamide (SP-10) reduces HIV-1 infectivity in vitro by modifying actin dynamics. benzamide 4-13 acrosomal vesicle protein 1 Homo sapiens 148-153 16364640-4 2006 Several compounds containing bulky lipophilic substituents at the benzamide pharmacophore yielded 10- to 17-fold selectivity for the VEGFR-2 versus VEGFR-1 kinase. benzamide 66-75 kinase insert domain receptor Homo sapiens 133-140 16364640-4 2006 Several compounds containing bulky lipophilic substituents at the benzamide pharmacophore yielded 10- to 17-fold selectivity for the VEGFR-2 versus VEGFR-1 kinase. benzamide 66-75 fms related receptor tyrosine kinase 1 Homo sapiens 148-155 17249247-3 2006 We investigated the in vitro efficacy, safety and mechanism of action of the benzamide derivative N-[1-(7-tert-Butyl-1H-indol-3-ylmethyl)-2-(4-cyclopropanecarbonyl-3-methyl-piperazin-1-yl)-2-oxo-ethyl]-4-nitro-benzamide (SP-10), a potential new HIV treatment. benzamide 77-86 acrosomal vesicle protein 1 Homo sapiens 221-226 16085414-1 2005 Several potent and efficacious MCHr1 antagonists containing an ortho-amino benzamide or nicotinamide chemotype have been identified, exemplified by 28 and 50. benzamide 75-84 melanin concentrating hormone receptor 1 Homo sapiens 31-36 16134937-2 2005 Novel 6-acylamino-2-aminoquinoline melanin-concentrating hormone 1 receptor (MCH1R) antagonists were identified by sequential in silico screening with 3D pharmacophore models derived from a series of benzamide antagonists. benzamide 200-209 melanin concentrating hormone receptor 1 Homo sapiens 35-75 16134937-2 2005 Novel 6-acylamino-2-aminoquinoline melanin-concentrating hormone 1 receptor (MCH1R) antagonists were identified by sequential in silico screening with 3D pharmacophore models derived from a series of benzamide antagonists. benzamide 200-209 melanin concentrating hormone receptor 1 Homo sapiens 77-82 16098204-8 2005 Further, in K562 cells, immunoprecipitation with the anti-TERT IgG and probed anti-poly (ADP-ribose) IgG revealed that TERT was poly(ADP-ribosyl)ated in the physiological condition of cell growth and such poly(ADP-ribosyl)ation was inhibited by benzamide treatment. benzamide 245-254 telomerase reverse transcriptase Homo sapiens 119-123 16098204-9 2005 Decrease in TEP1/TP1 expression and poly(ADP-ribosyl)ation of TERT were correlated with the inhibition of PARP activity by benzamide, indicating that PARP had a role in telomerase activity through poly(ADP-ribosyl)ation of TERT and down-regulation of TEP1/TP1. benzamide 123-132 telomerase protein component 1 Cricetulus griseus 12-16 16098204-9 2005 Decrease in TEP1/TP1 expression and poly(ADP-ribosyl)ation of TERT were correlated with the inhibition of PARP activity by benzamide, indicating that PARP had a role in telomerase activity through poly(ADP-ribosyl)ation of TERT and down-regulation of TEP1/TP1. benzamide 123-132 telomerase reverse transcriptase Cricetulus griseus 62-66 16098204-9 2005 Decrease in TEP1/TP1 expression and poly(ADP-ribosyl)ation of TERT were correlated with the inhibition of PARP activity by benzamide, indicating that PARP had a role in telomerase activity through poly(ADP-ribosyl)ation of TERT and down-regulation of TEP1/TP1. benzamide 123-132 poly [ADP-ribose] polymerase 1 Cricetulus griseus 106-110 16098204-9 2005 Decrease in TEP1/TP1 expression and poly(ADP-ribosyl)ation of TERT were correlated with the inhibition of PARP activity by benzamide, indicating that PARP had a role in telomerase activity through poly(ADP-ribosyl)ation of TERT and down-regulation of TEP1/TP1. benzamide 123-132 poly [ADP-ribose] polymerase 1 Cricetulus griseus 150-154 15740849-4 2005 MK-801 (NMDA receptor antagonist) as well as benzamide (PARP inhibitor), MDL 28170 (calpain inhibitor) and roscovitine (cyclin-dependent kinase inhibitor) inhibited the glutamate response to the YY1 complexes. benzamide 45-54 poly(ADP-ribose) polymerase 1 Homo sapiens 56-60 20711287-1 2005 BACKGROUND: Moclobemide, a benzamide, is one of the new-generation monoamine oxidase-A inhibitors (MAO-AIs) which belongs to the class of reversible inhibitors of monoamine oxidase (RIMA). benzamide 27-36 monoamine oxidase A Homo sapiens 67-86 15626725-10 2005 The regional selectivity of benzamide drugs (ampakines) may be explained, at least in part, by a lower potency at thalamic AMPA receptors, perhaps due to the prevalence of the subunits GluR3 and 4. benzamide 28-37 glutamate ionotropic receptor AMPA type subunit 3 Homo sapiens 185-196 15950463-1 2005 The identification of a novel series of benzamide-containing MCHr1 antagonists is described. benzamide 40-49 melanin-concentrating hormone receptor 1 Mus musculus 61-66 15740849-4 2005 MK-801 (NMDA receptor antagonist) as well as benzamide (PARP inhibitor), MDL 28170 (calpain inhibitor) and roscovitine (cyclin-dependent kinase inhibitor) inhibited the glutamate response to the YY1 complexes. benzamide 45-54 YY1 transcription factor Homo sapiens 195-198 16036766-5 2005 In the present paper the authors present their results using another benzamide with weak cholinesterase inhibitory properties, tiapride (TIA). benzamide 69-78 butyrylcholinesterase Homo sapiens 89-103 16178729-5 2005 The original compound in the benzamide series was discovered from screening and this series was optimized using an iterative library synthesis approach to explore SAR in each of three regions of the molecule. benzamide 29-38 sarcosine dehydrogenase Homo sapiens 163-166 16178729-7 2005 The pyrazole series used a fragment library approach based on small structural motives from the benzamide series to discover lead compounds and establish SAR. benzamide 96-105 sarcosine dehydrogenase Homo sapiens 154-157 15186837-4 2004 According to the docking simulation using the X-ray structure of EGFR kinase domain in complex with erlotinib, the LigScore2 scoring function value of erlotinib was calculated as 5.61, whereas that of the benzamide 1c was 5.05. benzamide 205-214 epidermal growth factor receptor Homo sapiens 65-69 15300712-1 2004 The benzamide compound metoclopramide (MCP) protects against cholinesterase inhibition by paraoxon (POX) both in vitro and in vivo. benzamide 4-13 butyrylcholinesterase Rattus norvegicus 61-75 15589979-12 2005 Finally, the PARP inhibitors benzamide and 6(5H)-phenanthridinone exerted notable inhibition of PARP activity and the nuclear translocation of the mitochondrial protein AIF (apoptosis-inducing factor) in MNNG-treated cells; however, these compounds exhibited no detectable inhibitory effects on MNNG-induced death in human lymphoblastoid cells. benzamide 29-38 poly(ADP-ribose) polymerase 1 Homo sapiens 13-17 15589979-12 2005 Finally, the PARP inhibitors benzamide and 6(5H)-phenanthridinone exerted notable inhibition of PARP activity and the nuclear translocation of the mitochondrial protein AIF (apoptosis-inducing factor) in MNNG-treated cells; however, these compounds exhibited no detectable inhibitory effects on MNNG-induced death in human lymphoblastoid cells. benzamide 29-38 poly(ADP-ribose) polymerase 1 Homo sapiens 96-100 15591342-4 2004 Moreover, embryonic trophoblast stem cell lines established from early PARG null embryos are viable only when cultured in medium containing the poly(ADP-ribose) polymerase inhibitor benzamide. benzamide 182-191 poly (ADP-ribose) glycohydrolase Mus musculus 71-75 15591342-4 2004 Moreover, embryonic trophoblast stem cell lines established from early PARG null embryos are viable only when cultured in medium containing the poly(ADP-ribose) polymerase inhibitor benzamide. benzamide 182-191 poly (ADP-ribose) polymerase family, member 1 Mus musculus 144-171 15591342-5 2004 Cells lacking PARG also show reduced growth, accumulation of PAR, and increased sensitivity to cytotoxicity induced by N-methyl-N"-nitro-N-nitrosoguanidine and menadione after benzamide withdrawal. benzamide 176-185 poly (ADP-ribose) glycohydrolase Mus musculus 14-18 15450410-1 2004 To investigate the effect of benzamide and nicotinamide, well known inhibitors of poly(ADP-ribose) polymerase, in Chinese hamster V79 cells at the physiological condition of cell growth, we have tested the ability of the inhibitors to induce apoptosis. benzamide 29-38 poly [ADP-ribose] polymerase 1 Cricetulus griseus 82-109 15450410-5 2004 However, 5 mM benzamide pre-treatment inhibited the nucleosomal ladders induced by gamma-irradiation indicating the role of poly(ADP-ribose) polymerase was different in irradiated cells and in un-irradiated cells. benzamide 14-23 poly [ADP-ribose] polymerase 1 Cricetulus griseus 124-151 14718597-4 2004 Structural analysis of one compound, a benzamide derivative, led to the identification of four related molecules, which are also OPG inducers. benzamide 39-48 TNF receptor superfamily member 11B Rattus norvegicus 129-132 14670625-0 2004 The PARP inhibitor benzamide protects against kainate and NMDA but not AMPA lesioning of the mouse striatum in vivo. benzamide 19-28 poly (ADP-ribose) polymerase family, member 1 Mus musculus 4-8 14670625-3 2004 Here, we have investigated the time-course of KA-induced toxicity and the effects of the PARP inhibitor benzamide on KA, AMPA and NMDA neurotoxicities in vivo, by measuring changes in the volume of the lesion and in NAD+ and ATP levels induced by the intra-striatal injection of these excitotoxins in C57Bl/6N mice. benzamide 104-113 poly (ADP-ribose) polymerase family, member 1 Mus musculus 89-93 14751292-3 2004 The present study examined three of these modulators for their effects on synaptic plasticity in field CA1 of hippocampal slices, two of them being the benzamide drugs 1-(quinoxalin-6-ylcarbonyl)piperidine (CX516) and 1-(1,4-benzodioxan-6-ylcarbonyl)piperidine (CX546) which prominently enhance synaptic transmission yet differ in their relative impact on amplitude versus duration of the synaptic response. benzamide 152-161 carbonic anhydrase 1 Homo sapiens 103-106 12643934-0 2003 Benzamide derivatives as blockers of Kv1.3 ion channel. benzamide 0-9 potassium voltage-gated channel subfamily A member 3 Homo sapiens 37-42 14969602-2 2003 Studies with a newer benzamide called 123I-epidepride, a high-affinity D2 receptor (D2R) antagonist, showed high sensitivity in D2R-positive pituitary adenomas. benzamide 21-30 dopamine receptor D2 Homo sapiens 71-82 14969602-2 2003 Studies with a newer benzamide called 123I-epidepride, a high-affinity D2 receptor (D2R) antagonist, showed high sensitivity in D2R-positive pituitary adenomas. benzamide 21-30 dopamine receptor D2 Homo sapiens 84-87 14969602-2 2003 Studies with a newer benzamide called 123I-epidepride, a high-affinity D2 receptor (D2R) antagonist, showed high sensitivity in D2R-positive pituitary adenomas. benzamide 21-30 dopamine receptor D2 Homo sapiens 128-131 12617906-0 2003 Cyclic amidines as benzamide bioisosteres: EPC synthesis and SAR studies leading to the selective dopamine D4 receptor agonist FAUC 312. benzamide 19-28 dopamine receptor D4 Homo sapiens 98-118 12617906-1 2003 Investigation of conformationally restricted benzamide bioisosteres led to the chiral phenyltetrahydropyrimidine derivative ent2a (FAUC 312) displaying strong and highly selective dopamine D4 receptor binding (K(i(high))=1.5 nM). benzamide 45-54 dopamine receptor D4 Homo sapiens 180-200 12643934-3 2003 A class of benzamide Kv1.3 channel inhibitors has been identified. benzamide 11-20 potassium voltage-gated channel subfamily A member 3 Homo sapiens 21-26 12459932-0 2003 On the protection against methamphetamine-induced neurotoxicity by benzamide, a PARP inhibitor. benzamide 67-76 poly(ADP-ribose) polymerase 1 Homo sapiens 80-84 12581860-7 2003 Furthermore, 3-aminobenzamide (3AB) and benzamide, inhibitors of poly (ADP-ribose) polymerase (PARP) that are activated upon recognition of DNA strand breaks, suppressed the further increase by gamma-irradiation in IFN-gamma-induced NO production and the I-kappaB degradation by gamma-irradiation. benzamide 20-29 poly (ADP-ribose) polymerase family, member 1 Mus musculus 65-93 12581860-7 2003 Furthermore, 3-aminobenzamide (3AB) and benzamide, inhibitors of poly (ADP-ribose) polymerase (PARP) that are activated upon recognition of DNA strand breaks, suppressed the further increase by gamma-irradiation in IFN-gamma-induced NO production and the I-kappaB degradation by gamma-irradiation. benzamide 20-29 poly (ADP-ribose) polymerase family, member 1 Mus musculus 95-99 12581860-7 2003 Furthermore, 3-aminobenzamide (3AB) and benzamide, inhibitors of poly (ADP-ribose) polymerase (PARP) that are activated upon recognition of DNA strand breaks, suppressed the further increase by gamma-irradiation in IFN-gamma-induced NO production and the I-kappaB degradation by gamma-irradiation. benzamide 20-29 interferon gamma Mus musculus 215-224 12165366-1 2002 The aim of the study was to examine the action of low-dose amisulpride (100 mg/d), an atypical antipsychotic from the benzamide class with a high affinity for the D2 and D3 dopamine receptors, given for 4 weeks in 19 schizophrenic patients with the deficit syndrome, in terms of clinical response, modifications in their cognitive performance and changes in brain perfusion values. benzamide 118-127 dopamine receptor D2 Homo sapiens 163-204 12464646-10 2002 Structure-function analysis indicated that the induction of apoptosis by compounds derived from COX-2 inhibitors required a bulky terminal phenyl ring, a heterocyclic system with negative electrostatic potential, and a benzenesulfonamide or benzenecarboxamide moiety. benzamide 241-259 prostaglandin-endoperoxide synthase 2 Homo sapiens 96-101 12411406-6 2002 Both 6(5H)-phenanthridinone and benzamide attenuated development of EAE, reducing clinical score, neuroimmune infiltration and expression of inflammatory mediators such as inducible nitric oxide synthase, interleukin-1beta and -2, cyclooxygenase-2, tumour necrosis factor-alpha and interferon-gamma in the spinal cord of myelin-immunized rats. benzamide 32-41 interleukin 1 beta Rattus norvegicus 205-229 12411406-6 2002 Both 6(5H)-phenanthridinone and benzamide attenuated development of EAE, reducing clinical score, neuroimmune infiltration and expression of inflammatory mediators such as inducible nitric oxide synthase, interleukin-1beta and -2, cyclooxygenase-2, tumour necrosis factor-alpha and interferon-gamma in the spinal cord of myelin-immunized rats. benzamide 32-41 prostaglandin-endoperoxide synthase 2 Rattus norvegicus 231-277 12411406-6 2002 Both 6(5H)-phenanthridinone and benzamide attenuated development of EAE, reducing clinical score, neuroimmune infiltration and expression of inflammatory mediators such as inducible nitric oxide synthase, interleukin-1beta and -2, cyclooxygenase-2, tumour necrosis factor-alpha and interferon-gamma in the spinal cord of myelin-immunized rats. benzamide 32-41 interferon gamma Rattus norvegicus 282-298 12411406-10 2002 In cultures of activated rat lymphocytes, 6(5H)-phenanthridinone and benzamide reduced the DNA-binding activity of NF-kappaB and AP-1 and transcription of pro-inflammatory cytokines such as interleukin-2, interferon-gamma and tumour necrosis factor-alpha. benzamide 69-78 Jun proto-oncogene, AP-1 transcription factor subunit Rattus norvegicus 129-133 12411406-10 2002 In cultures of activated rat lymphocytes, 6(5H)-phenanthridinone and benzamide reduced the DNA-binding activity of NF-kappaB and AP-1 and transcription of pro-inflammatory cytokines such as interleukin-2, interferon-gamma and tumour necrosis factor-alpha. benzamide 69-78 interleukin 2 Rattus norvegicus 190-203 12411406-10 2002 In cultures of activated rat lymphocytes, 6(5H)-phenanthridinone and benzamide reduced the DNA-binding activity of NF-kappaB and AP-1 and transcription of pro-inflammatory cytokines such as interleukin-2, interferon-gamma and tumour necrosis factor-alpha. benzamide 69-78 interferon gamma Rattus norvegicus 205-254 11823129-1 2002 Two benzamide derivatives as dopamine D4 receptor antagonists, YM-50001(4) and N- [2-[4-(4-chlorophenyl]piperizin-1-yl]ethyl]-3-methoxybenzamide (9), were labeled by positron-emitter (11C), and their pharmacological specificities to dopamine D4 receptors were examined by quantitative autoradiography and positron emission tomography (PET). benzamide 4-13 dopamine receptor D4 Rattus norvegicus 29-49 12207145-0 2002 Long-term effects of the substituted benzamide derivative amisulpride on baseline and stimulated prolactin levels. benzamide 37-46 prolactin Homo sapiens 97-106 11593040-6 2001 Cell death in each condition was markedly reduced by the PARP1 inhibitor benzamide and equally reduced by the PARG inhibitors gallotannin and nobotanin B. benzamide 73-82 poly (ADP-ribose) polymerase family, member 1 Mus musculus 57-62 11593040-7 2001 The PARP1 inhibitor benzamide and the PARG inhibitor gallotannin both prevented the NAD(+) depletion that otherwise results from PARP1 activation by MNNG or H(2)O(2). benzamide 20-29 poly (ADP-ribose) polymerase family, member 1 Mus musculus 4-9 11593040-7 2001 The PARP1 inhibitor benzamide and the PARG inhibitor gallotannin both prevented the NAD(+) depletion that otherwise results from PARP1 activation by MNNG or H(2)O(2). benzamide 20-29 poly (ADP-ribose) polymerase family, member 1 Mus musculus 129-134 11562279-11 2001 The benzamide MS-275 belongs to a new class of synthetic HDAC inhibitors and displays oral activity in animal models. benzamide 4-13 histone deacetylase 9 Homo sapiens 57-61 15995937-2 2001 Early designs of PARP inhibitors were primarily based on mimicking the structure of nicotinamide and resulted in the identification and widespread use of benzamide analogs as PARP inhibitors. benzamide 154-163 poly(ADP-ribose) polymerase 1 Homo sapiens 17-21 11549463-0 2001 Benzamide bioisosteres incorporating dihydroheteroazole substructures: EPC synthesis and SAR leading to a selective dopamine D4 receptor partial agonist (FAUC 179). benzamide 0-9 sarcosine dehydrogenase Homo sapiens 89-92 11549463-0 2001 Benzamide bioisosteres incorporating dihydroheteroazole substructures: EPC synthesis and SAR leading to a selective dopamine D4 receptor partial agonist (FAUC 179). benzamide 0-9 dopamine receptor D4 Homo sapiens 116-136 11549463-1 2001 Conformationally restricted benzamide bioisosteres were investigated when the chiral phenyldihydroimidazole derivative 4e (FAUC 179) showed strong and highly selective dopamine D4 receptor binding (K(i)high=0.95nM). benzamide 28-37 dopamine receptor D4 Homo sapiens 168-188 15995937-2 2001 Early designs of PARP inhibitors were primarily based on mimicking the structure of nicotinamide and resulted in the identification and widespread use of benzamide analogs as PARP inhibitors. benzamide 154-163 poly(ADP-ribose) polymerase 1 Homo sapiens 175-179 10822064-3 2000 In the present study, the antiarrhythmic activity of Benzamide, N-(aminoiminomethyl)-4-?4-(2-furanylcarbonyl)-1-piperazinyl -3-(methy lsulfonyl), methanesulfonate (BIIB 513), a novel NHE-1 inhibitor, was examined. benzamide 53-62 solute carrier family 9 member A1 Canis lupus familiaris 183-188 11331359-9 2001 Finally, we observed that DTDP toxicity could be blocked with niacinamide or benzamide, inhibitors of poly (ADP-ribose) synthetase. benzamide 77-86 poly(ADP-ribose) polymerase 1 Homo sapiens 102-130 10869705-6 2000 Coperfusion of SNAP with the free radical scavengers superoxide dismutase (SOD; 60 microg/ml) and catalase (50 microg/ml) reduced or eliminated the ability of the NO-donor to enhance [3H]purine release, but the poly (ADP-ribosyl) synthetase (PARS) inhibitor benzamide (500 microM) did not affect it. benzamide 258-267 catalase Homo sapiens 75-106 11049868-4 2000 Intraperitoneal administration of PARP inhibitors, benzamide or 3-amino benzamide, after I/R injury accelerates the recovery of normal renal function, as assessed by monitoring the levels of plasma creatinine and blood urea nitrogen during 6 days postischemia. benzamide 51-60 poly (ADP-ribose) polymerase 1 Rattus norvegicus 34-38 10841343-5 2000 Gallotannin was more than 10-fold more potent than the PARP inhibitor benzamide in preventing H2O2-induced cell death. benzamide 70-79 poly (ADP-ribose) polymerase family, member 1 Mus musculus 55-59 10719223-3 2000 Compared to the long form of the D2 receptor (D2(Long)), the short form (D2(Short)) may be three times more sensitive to benzamide antipsychotic drugs. benzamide 121-130 immunoglobulin heavy diversity 2-15 Homo sapiens 46-54 10704772-7 2000 We now report potent inhibition of p38-MAPK phosphorylation by a synthetic benzamide (CPI-1189) which displays protective action against tumor necrosis factor-alpha (TNFalpha)-induced neurodegeneration. benzamide 75-84 mitogen-activated protein kinase 14 Homo sapiens 35-38 10704772-7 2000 We now report potent inhibition of p38-MAPK phosphorylation by a synthetic benzamide (CPI-1189) which displays protective action against tumor necrosis factor-alpha (TNFalpha)-induced neurodegeneration. benzamide 75-84 tumor necrosis factor Homo sapiens 137-164 10704772-7 2000 We now report potent inhibition of p38-MAPK phosphorylation by a synthetic benzamide (CPI-1189) which displays protective action against tumor necrosis factor-alpha (TNFalpha)-induced neurodegeneration. benzamide 75-84 tumor necrosis factor Homo sapiens 166-174 10200742-2 1999 OBJECTIVE: The goal of this placebo-controlled study was to evaluate the efficacy and safety of low doses of amisulpride, an atypical antipsychotic of the benzamide class with high affinity for D2 and D3 dopamine receptors, in the treatment of schizophrenic patients with predominantly primary negative symptoms. benzamide 155-164 dopamine receptor D2 Homo sapiens 194-222 10649982-1 2000 N-[2-[4-(4-Chlorophenyl)piperazin-1-yl]ethyl]-3-methoxybenzamide (1), a high-affinity and selective dopamine D(4) receptor ligand, was chosen as a lead, and structural modifications were done on its amide bond and on its alkyl chain linking the benzamide moiety to the piperazine ring and by preparing some semirigid analogues. benzamide 55-64 dopamine receptor D4 Homo sapiens 100-122 10647912-4 1999 Ecabapide mainly underwent N-dealkylation to form M1 and 6-hydroxylation of the benzamide moiety to form M6. benzamide 80-89 cholinergic receptor muscarinic 1 Homo sapiens 50-58 16414805-1 1998 Moclobemide, a benzamide derivative, predominantly inhibits the A form of monoamine oxidase (MAO) and its MAO binding is reversible. benzamide 15-24 monoamine oxidase A Rattus norvegicus 74-91 10668429-1 1999 Decreases in mouse brain NAD+ and ATP caused by MPTP are prevented by the PARP inhibitor benzamide. benzamide 89-98 poly (ADP-ribose) polymerase family, member 1 Mus musculus 74-78 9453543-7 1998 Several PARP inhibitors [benzamide, 3-aminobenzamide, nicotinamide, and 6(5H)-phenanthridinone] prevented cell death, but the inactive analogue benzoic acid did not. benzamide 25-34 poly (ADP-ribose) polymerase family, member 1 Mus musculus 8-12 10668429-5 1999 The results confirm that MPTP reduces striatal ATP levels, as previously reported by Chan et al., show that MPTP causes a regionally-selective (striatal and midbrain) loss of NAD+, and indicate that the PARP inhibitor benzamide can prevent these losses without interfering with MPTP-induced striatal dopamine release. benzamide 218-227 poly (ADP-ribose) polymerase family, member 1 Mus musculus 203-207 9795136-0 1998 Decreases in mouse brain NAD+ and ATP induced by 1-methyl-4-phenyl-1, 2,3,6-tetrahydropyridine (MPTP): prevention by the poly(ADP-ribose) polymerase inhibitor, benzamide. benzamide 160-169 poly (ADP-ribose) polymerase family, member 1 Mus musculus 121-148 9795136-1 1998 Inhibitors of poly(ADP-ribose) polymerase (PARP), including benzamide, protect against 1-methyl-4-phenyl-1,2,3, 6-tetrahydropyridine (MPTP)-induced dopamine neurotoxicity in vivo [Cosi et al., Brain Res. benzamide 60-69 poly (ADP-ribose) polymerase family, member 1 Mus musculus 14-41 9795136-1 1998 Inhibitors of poly(ADP-ribose) polymerase (PARP), including benzamide, protect against 1-methyl-4-phenyl-1,2,3, 6-tetrahydropyridine (MPTP)-induced dopamine neurotoxicity in vivo [Cosi et al., Brain Res. benzamide 60-69 poly (ADP-ribose) polymerase family, member 1 Mus musculus 43-47 9795136-14 1998 ]; (2) show that MPTP causes a regionally-dependent (striatal and midbrain) loss of NAD+; (3) indicate that the PARP inhibitor benzamide can prevent these losses without interfering with MPTP-induced striatal dopamine release; and (4) provide further evidence to suggest an involvement of PARP in MPTP-induced neurotoxicity in vivo. benzamide 127-136 poly (ADP-ribose) polymerase family, member 1 Mus musculus 112-116 9795136-14 1998 ]; (2) show that MPTP causes a regionally-dependent (striatal and midbrain) loss of NAD+; (3) indicate that the PARP inhibitor benzamide can prevent these losses without interfering with MPTP-induced striatal dopamine release; and (4) provide further evidence to suggest an involvement of PARP in MPTP-induced neurotoxicity in vivo. benzamide 127-136 poly (ADP-ribose) polymerase family, member 1 Mus musculus 289-293 16414805-1 1998 Moclobemide, a benzamide derivative, predominantly inhibits the A form of monoamine oxidase (MAO) and its MAO binding is reversible. benzamide 15-24 monoamine oxidase A Rattus norvegicus 93-96 16414805-1 1998 Moclobemide, a benzamide derivative, predominantly inhibits the A form of monoamine oxidase (MAO) and its MAO binding is reversible. benzamide 15-24 monoamine oxidase A Rattus norvegicus 106-109 9336344-0 1997 An anti-inflammatory benzamide derivative inhibits the protein kinase C (PKC)-dependent pathway of ERK2 phosphorylation in murine macrophages. benzamide 21-30 mitogen-activated protein kinase 1 Mus musculus 99-103 9336344-1 1997 We have previously described benzamide derivatives that inhibited tumor necrosis factor (TNF) production from activated macrophages (Mphi) probably by interacting with a protein kinase C (PKC)-dependent pathway. benzamide 29-38 tumor necrosis factor Mus musculus 66-87 9336344-1 1997 We have previously described benzamide derivatives that inhibited tumor necrosis factor (TNF) production from activated macrophages (Mphi) probably by interacting with a protein kinase C (PKC)-dependent pathway. benzamide 29-38 tumor necrosis factor Mus musculus 89-92 9364937-2 1997 Other chemicals, such as benzamide, colchicine, thiamphenicol and paracetamol, that are already known to specifically induce transcription at the hsr omega locus are also identified as amides. benzamide 25-34 Heat shock RNA omega Drosophila melanogaster 146-155 9364937-3 1997 In view of the specific induction of the 93D puff by different amides and other data that demonstrate hsr omega transcription in response to benzamide and colchicine etc. benzamide 141-150 Heat shock RNA omega Drosophila melanogaster 102-111 10638823-1 1996 The purpose of the present set of studies was to characterize, in vitro and in vivo, two benzamide analogues, 2,3-dimethoxy-N-[1-(4-fluorobenzyl)piperidin4yl]benzamide (MBP) and 4"-fluoroclebopride (FCP), for studying dopamine D2 receptors with Positron Emission Tomography (PET). benzamide 89-98 myelin basic protein Macaca mulatta 169-172 9271347-6 1997 Moreover, combined treatment of cells with TZM and benzamide, an inhibitor of the poly(ADP-ribose) polymerase (EC 2.4.2.30), increased the apoptosis induced by the methylating agent. benzamide 51-60 poly(ADP-ribose) polymerase 1 Homo sapiens 82-109 9166736-10 1997 In contrast, BDP-37, a member of the benzamide family of drugs, exhibited a lower potency for GluR2 flip (58 microM) than for any of the flop isoforms (18-40 microM). benzamide 37-46 glutamate ionotropic receptor AMPA type subunit 2 Homo sapiens 94-99 9226586-1 1997 Mosapride citrate, a novel benzamide-type gastroprokinetic agent, is clinically prescribed as a racemate and is metabolized to its des-4-fluorobenzyl structure (M-1). benzamide 27-36 myoregulin Homo sapiens 161-164 9212448-0 1997 New benzamide-derived 5-HT3 receptor antagonists which prevent the effects of ethanol on extracellular dopamine, and fail to reduce voluntary alcohol intake in rats. benzamide 4-13 5-hydroxytryptamine receptor 3A Rattus norvegicus 22-36 8742516-5 1996 While the PARP-activity remained essentially unchanged, the acetaminophen-induced release of both GOT and GPT from injured liver cells could be inhibited by 90-99%, when mice were injected additionally with the selective PARP-inhibitors nicotinic acid amide, benzamide, caffeine, theophyline, and thymidine, respectively. benzamide 259-268 glutamic pyruvic transaminase, soluble Mus musculus 106-109 8911677-0 1996 Benzamide, an inhibitor of poly(ADP-ribose) polymerase, attenuates methamphetamine-induced dopamine neurotoxicity in the C57B1/6N mouse. benzamide 0-9 poly (ADP-ribose) polymerase family, member 1 Mus musculus 27-54 8911677-1 1996 Previous studies have indicated that the activation of poly(ADP-ribose) polymerase (PARP), an enzyme involved in DNA plasticity-related phenomena, is an early event occurring in glutamate-induced neurotoxicity in vitro, and that inhibitors of PARP, including benzamide, are protective against both glutamate- and methamphetamine (METH)-induced neurotoxicity in vitro. benzamide 259-268 poly (ADP-ribose) polymerase family, member 1 Mus musculus 55-82 8911677-1 1996 Previous studies have indicated that the activation of poly(ADP-ribose) polymerase (PARP), an enzyme involved in DNA plasticity-related phenomena, is an early event occurring in glutamate-induced neurotoxicity in vitro, and that inhibitors of PARP, including benzamide, are protective against both glutamate- and methamphetamine (METH)-induced neurotoxicity in vitro. benzamide 259-268 poly (ADP-ribose) polymerase family, member 1 Mus musculus 84-88 8911677-7 1996 The concentrations of benzamide measured in the striatum at different times following this same dose of drug were in a range (0.09-0.64 mM) reported in in vitro studies to be both neuroprotective and effective in inhibiting PARP activity. benzamide 22-31 poly (ADP-ribose) polymerase family, member 1 Mus musculus 224-228 8809159-5 1996 Further, the beta 2-AR can accommodate larger substituents such as a benzamide at the 4"-position (26b). benzamide 69-78 adrenoceptor beta 2 Homo sapiens 13-22 8876997-2 1996 Co-treatments with five different inhibitors of poly(ADP-ribose) polymerase (PARP), including benzamide, significantly prevented the MPTP-induced catecholamine depletions. benzamide 94-103 poly (ADP-ribose) polymerase family, member 1 Mus musculus 48-75 8876997-2 1996 Co-treatments with five different inhibitors of poly(ADP-ribose) polymerase (PARP), including benzamide, significantly prevented the MPTP-induced catecholamine depletions. benzamide 94-103 poly (ADP-ribose) polymerase family, member 1 Mus musculus 77-81 8876997-5 1996 The protective activities of benzamide and its derivatives paralleled their in vitro efficacies and potencies both as neuroprotective agents and as inhibitors of PARP, while the activity of 1,5-dihydroxyisoquinoline, a structurally-unrelated compound, did not. benzamide 29-38 poly (ADP-ribose) polymerase family, member 1 Mus musculus 162-166 8981558-1 1996 Inhibitory effects of the dopamine D2-receptor antagonistic benzamide compound metoclopramide (MCP) on acetylcholinesterase (AChE; EC 3.1.1.7) isoenzymes of both erythrocytes and human caudate nucleus and on human serum cholinesterase (ChE; EC 3.1.1.8) were studied in vitro using a spectrophotometric assay with acetylthiocholine (ASCh) as substrate. benzamide 60-69 dopamine receptor D2 Homo sapiens 26-46 8981558-1 1996 Inhibitory effects of the dopamine D2-receptor antagonistic benzamide compound metoclopramide (MCP) on acetylcholinesterase (AChE; EC 3.1.1.7) isoenzymes of both erythrocytes and human caudate nucleus and on human serum cholinesterase (ChE; EC 3.1.1.8) were studied in vitro using a spectrophotometric assay with acetylthiocholine (ASCh) as substrate. benzamide 60-69 acetylcholinesterase (Cartwright blood group) Homo sapiens 103-123 8981558-1 1996 Inhibitory effects of the dopamine D2-receptor antagonistic benzamide compound metoclopramide (MCP) on acetylcholinesterase (AChE; EC 3.1.1.7) isoenzymes of both erythrocytes and human caudate nucleus and on human serum cholinesterase (ChE; EC 3.1.1.8) were studied in vitro using a spectrophotometric assay with acetylthiocholine (ASCh) as substrate. benzamide 60-69 acetylcholinesterase (Cartwright blood group) Homo sapiens 125-129 8981558-1 1996 Inhibitory effects of the dopamine D2-receptor antagonistic benzamide compound metoclopramide (MCP) on acetylcholinesterase (AChE; EC 3.1.1.7) isoenzymes of both erythrocytes and human caudate nucleus and on human serum cholinesterase (ChE; EC 3.1.1.8) were studied in vitro using a spectrophotometric assay with acetylthiocholine (ASCh) as substrate. benzamide 60-69 butyrylcholinesterase Homo sapiens 109-123 8981558-1 1996 Inhibitory effects of the dopamine D2-receptor antagonistic benzamide compound metoclopramide (MCP) on acetylcholinesterase (AChE; EC 3.1.1.7) isoenzymes of both erythrocytes and human caudate nucleus and on human serum cholinesterase (ChE; EC 3.1.1.8) were studied in vitro using a spectrophotometric assay with acetylthiocholine (ASCh) as substrate. benzamide 60-69 butyrylcholinesterase Homo sapiens 126-129 9081862-1 1996 The 93D, or hsr-omega (heat-shock RNA-omega), locus of Drosophila melanogaster and other species of Drosophila, besides being induced as a member of the heat shock gene family, is also selectively and singularly inducible by a variety of agents, notably benzamide, colchicine and vitamin B6 (in species other than D. melanogaster). benzamide 254-263 Heat shock RNA omega Drosophila melanogaster 12-21 8569793-0 1996 Reversion in Chinese hamster lines amplified at the AMPD2 locus: spontaneous and benzamide-stimulated gradual loss of amplified alleles of marker genes. benzamide 81-90 AMP deaminase 2 Cricetulus griseus 52-57 8742516-5 1996 While the PARP-activity remained essentially unchanged, the acetaminophen-induced release of both GOT and GPT from injured liver cells could be inhibited by 90-99%, when mice were injected additionally with the selective PARP-inhibitors nicotinic acid amide, benzamide, caffeine, theophyline, and thymidine, respectively. benzamide 259-268 poly (ADP-ribose) polymerase family, member 1 Mus musculus 221-225 7562546-6 1995 More likely, these benzamide derivatives acted mainly at the level of the protein kinase C (PKC) pathway because: 1) After treatment of M phi with PKC inhibitors which significantly inhibited TNF production, our compounds showed no additional inhibition. benzamide 19-28 tumor necrosis factor Homo sapiens 192-195 8135490-8 1993 It has structural resemblance to some of the known inhibitors of the DNA associated enzyme poly ADPRT such as benzamide. benzamide 110-119 ADP-ribosyltransferase 1 Mus musculus 96-101 7562546-4 1995 We show that, in marked contrast with ibuprofen, flurbiprofen and indomethacin which all significantly enhanced TNF production, the two benzamide derivatives tested, JM34 and JM42, significantly inhibited TNF-alpha production by zymosan or lipopolysaccharide-activated M phi. benzamide 136-145 tumor necrosis factor Homo sapiens 205-214 8038764-0 1994 Synthesis of 11C-labelled benzamide compounds as potential tracers for poly(ADP-ribose) synthetase. benzamide 26-35 poly(ADP-ribose) polymerase 1 Homo sapiens 71-98 8145235-3 1994 Replacement of the benzamide portion of the (p-aminobenzoyl)glutamate moiety with 2-fluorobenzamido, 2-isoindolinyl, 1,2-benzisothiazol-2-yl, and 2-thenamido moieties varied in effect from a 9-fold diminution of TS activity to a 5-fold enhancement, while cytotoxic potency on SW-480 and MCF-7 tumor lines showed increases ranging from 3.6- to 450-fold. benzamide 19-28 thymidylate synthetase Homo sapiens 212-214 7553982-4 1995 Among them, some benzamide derivatives having a 1,4-diazepine ring showed a potent 5-HT3 receptor antagonistic activity. benzamide 17-26 5-hydroxytryptamine receptor 3A Rattus norvegicus 83-97 7540096-2 1995 While heat shock increased the levels of all the three transcripts at the 93D puff site in a coordinated manner, benzamide led to a significant increase in the levels of hsr-omega-n and pre-c; on the other hand, colchicine caused increased levels of the omega-n and omega-c RNA species at 93D. benzamide 113-122 Heat shock RNA omega Drosophila melanogaster 170-181 7540096-5 1995 Although a combined treatment to salivary glands with heat shock and benzamide or colchicine is known to inhibit puffing and [3H]uridine incorporation at 93D, the two treatments resulted in a treatment-specific increase in the in situ levels of different hsr-omega transcripts at the 93D site, suggesting a reduced turnover of specific transcripts from the site under these conditions. benzamide 69-78 Heat shock RNA omega Drosophila melanogaster 255-264 8306827-5 1993 The association of HSP90 with the 93D locus was strictly heat shock dependent as shown by the absence of HSP90 in puff 93D induced by either benzamide or colchicine. benzamide 141-150 Heat shock protein 83 Drosophila melanogaster 19-24 7690896-3 1993 A similar important role of BrdUrd in SCE induction has been reported in the cases of benzamide (BA) (Natarajan et al., 1981) and camptothecin (CPT) (Zhao et al., 1992), which are inhibitors of poly(ADP-ribose)polymerase and DNA topoisomerase I (topo I), respectively. benzamide 86-95 poly(ADP-ribose) polymerase 1 Homo sapiens 194-220 7690896-3 1993 A similar important role of BrdUrd in SCE induction has been reported in the cases of benzamide (BA) (Natarajan et al., 1981) and camptothecin (CPT) (Zhao et al., 1992), which are inhibitors of poly(ADP-ribose)polymerase and DNA topoisomerase I (topo I), respectively. benzamide 97-99 poly(ADP-ribose) polymerase 1 Homo sapiens 194-220 8255982-2 1993 Moclobemide is a novel benzamide reversible inhibitor of monoamine oxidase A and has clinical efficacy in a wide spectrum of depressive illness including endogenous and non-endogenous depression, in younger adults and in the elderly. benzamide 23-32 monoamine oxidase A Homo sapiens 57-76 8241609-2 1993 Tiapride is a substituted benzamide derivative with selective dopamine D2-receptor antagonist properties which appears to have preferential affinity for extrastriatal dopamine receptors. benzamide 26-35 dopamine receptor D2 Homo sapiens 62-82 8347172-5 1993 ABA and BA inhibited the activity of poly(ADP-ribose) polymerase by 85%. benzamide 1-3 poly (ADP-ribose) polymerase family, member 1 Mus musculus 37-64 8347172-12 1993 With the cultured hepatocytes, ABA and BA inhibited poly(ADP-ribose) polymerase at concentrations that were without effect on either the extent of cell killing or the depletion of NAD occurring with either TBHP, H2O2, or menadione. benzamide 32-34 poly (ADP-ribose) polymerase family, member 1 Mus musculus 52-79 8232288-0 1993 Characterization of the superinduction of the c-myc proto-oncogene in fibroblasts by benzamide derivatives. benzamide 85-94 myelocytomatosis oncogene Mus musculus 46-66 1535660-0 1992 Conformational analysis of dopamine D-2 receptor antagonists of the benzamide series in relation to a recently proposed D-2 receptor-interaction model. benzamide 68-77 dopamine receptor D2 Homo sapiens 27-48 7682390-2 1993 Both this ADP-ribosylation reaction and granulocytic differentiation in response to recombinant G-CSF were inhibited approximately 50% by 2 mM benzamide, suggesting a correlation between these two processes. benzamide 143-152 peripheral blood stem cell response to granulocyte colony stimulating factor 1 Mus musculus 96-101 1327852-5 1992 A range of competitive inhibitors (benzamide and its derivatives) of the nuclear enzyme poly(ADP-ribose) polymerase (PADPRP; EC 2.4.2.30) was utilized, and their ability to induce melanogenesis reflected their potency as PADPRP inhibitors. benzamide 35-44 poly (ADP-ribose) polymerase family, member 1 Mus musculus 88-115 1327852-5 1992 A range of competitive inhibitors (benzamide and its derivatives) of the nuclear enzyme poly(ADP-ribose) polymerase (PADPRP; EC 2.4.2.30) was utilized, and their ability to induce melanogenesis reflected their potency as PADPRP inhibitors. benzamide 35-44 poly (ADP-ribose) polymerase family, member 1 Mus musculus 117-123 1327852-5 1992 A range of competitive inhibitors (benzamide and its derivatives) of the nuclear enzyme poly(ADP-ribose) polymerase (PADPRP; EC 2.4.2.30) was utilized, and their ability to induce melanogenesis reflected their potency as PADPRP inhibitors. benzamide 35-44 poly (ADP-ribose) polymerase family, member 1 Mus musculus 221-227 1394694-0 1992 Synthesis and evaluation of iodinated benzamide derivatives as selective and reversible monoamine oxidase B inhibitors. benzamide 38-47 monoamine oxidase B Homo sapiens 88-107 1617671-6 1992 The inhibitors of ADP-ribose transferase benzamide and 3-amino-benzamide suppressed the elongation of the c-fos message and the de novo synthesis of nuclear factors, among them c-Fos and c-Jun, which bind to the fos-AP-1 motif in vitro only following stimulation with active oxygen. benzamide 41-50 FBJ osteosarcoma oncogene Mus musculus 106-111 1617671-6 1992 The inhibitors of ADP-ribose transferase benzamide and 3-amino-benzamide suppressed the elongation of the c-fos message and the de novo synthesis of nuclear factors, among them c-Fos and c-Jun, which bind to the fos-AP-1 motif in vitro only following stimulation with active oxygen. benzamide 41-50 FBJ osteosarcoma oncogene Mus musculus 177-182 1617671-6 1992 The inhibitors of ADP-ribose transferase benzamide and 3-amino-benzamide suppressed the elongation of the c-fos message and the de novo synthesis of nuclear factors, among them c-Fos and c-Jun, which bind to the fos-AP-1 motif in vitro only following stimulation with active oxygen. benzamide 41-50 jun proto-oncogene Mus musculus 187-192 1617671-6 1992 The inhibitors of ADP-ribose transferase benzamide and 3-amino-benzamide suppressed the elongation of the c-fos message and the de novo synthesis of nuclear factors, among them c-Fos and c-Jun, which bind to the fos-AP-1 motif in vitro only following stimulation with active oxygen. benzamide 41-50 FBJ osteosarcoma oncogene Mus musculus 108-111 1773788-1 1991 A poly(ADP-ribose) polymerase inhibitor, benzamide (BA), was found to induce flat revertants of NIH 3T3 cells that had been transformed by human Ha-ras, rat Ki-ras, rat c-raf, and human ret-II. benzamide 41-50 poly(ADP-ribose) polymerase 1 Homo sapiens 2-29 1660277-3 1991 The amplified catalase and c-myc genes in HP100-1 cells were not decreased by treatment of the cells with inhibitors of poly(ADP-Ribose) polymerase, such as nicotinamide and benzamide. benzamide 174-183 MYC proto-oncogene, bHLH transcription factor Homo sapiens 27-32 1773788-1 1991 A poly(ADP-ribose) polymerase inhibitor, benzamide (BA), was found to induce flat revertants of NIH 3T3 cells that had been transformed by human Ha-ras, rat Ki-ras, rat c-raf, and human ret-II. benzamide 41-50 KRAS proto-oncogene, GTPase Rattus norvegicus 157-163 1773788-1 1991 A poly(ADP-ribose) polymerase inhibitor, benzamide (BA), was found to induce flat revertants of NIH 3T3 cells that had been transformed by human Ha-ras, rat Ki-ras, rat c-raf, and human ret-II. benzamide 41-50 Raf-1 proto-oncogene, serine/threonine kinase Rattus norvegicus 169-174 1773788-1 1991 A poly(ADP-ribose) polymerase inhibitor, benzamide (BA), was found to induce flat revertants of NIH 3T3 cells that had been transformed by human Ha-ras, rat Ki-ras, rat c-raf, and human ret-II. benzamide 41-50 golgin A5 Homo sapiens 186-192 1773788-1 1991 A poly(ADP-ribose) polymerase inhibitor, benzamide (BA), was found to induce flat revertants of NIH 3T3 cells that had been transformed by human Ha-ras, rat Ki-ras, rat c-raf, and human ret-II. benzamide 52-54 poly(ADP-ribose) polymerase 1 Homo sapiens 2-29 1773788-1 1991 A poly(ADP-ribose) polymerase inhibitor, benzamide (BA), was found to induce flat revertants of NIH 3T3 cells that had been transformed by human Ha-ras, rat Ki-ras, rat c-raf, and human ret-II. benzamide 52-54 KRAS proto-oncogene, GTPase Rattus norvegicus 157-163 1773788-1 1991 A poly(ADP-ribose) polymerase inhibitor, benzamide (BA), was found to induce flat revertants of NIH 3T3 cells that had been transformed by human Ha-ras, rat Ki-ras, rat c-raf, and human ret-II. benzamide 52-54 Raf-1 proto-oncogene, serine/threonine kinase Rattus norvegicus 169-174 1773788-1 1991 A poly(ADP-ribose) polymerase inhibitor, benzamide (BA), was found to induce flat revertants of NIH 3T3 cells that had been transformed by human Ha-ras, rat Ki-ras, rat c-raf, and human ret-II. benzamide 52-54 golgin A5 Homo sapiens 186-192 1901170-3 1991 Two inhibitors of ADPRT, benzamide, competing with NAD at the nicotinamide binding site, and 6-amino-1,2-benzopyrone, which competes with DNA at the DNA binding site(s), both selectively arrest differentiation at the prodissoconch stage. benzamide 25-34 poly [ADP-ribose] polymerase 1 Bos taurus 18-23 2139420-9 1990 Inhibitors of ADPRT, nicotinamide, caffeine and benzamide inhibited the induction of ODC by PHA in a concentration-dependent manner, in the range (0.6-10 mM) known to inhibit ADPRT. benzamide 48-57 ornithine decarboxylase 1 Homo sapiens 85-88 2144583-9 1990 It is concluded that the D2 dopamine receptor binding site contains separate but over-lapping binding regions for antagonists such as spiperone and substituted benzamide drugs. benzamide 160-169 dopamine receptor D2 Homo sapiens 25-45 2123732-5 1990 Following treatment of these cells with 2 mM benzamide, an inhibitor of the NAD(+)-utilizing enzyme poly(ADP-ribose) polymerase, NAD+ levels slowly increased up to about 160% of control levels after 3 hours. benzamide 45-54 poly (ADP-ribose) polymerase family, member 1 Mus musculus 100-127 2139420-9 1990 Inhibitors of ADPRT, nicotinamide, caffeine and benzamide inhibited the induction of ODC by PHA in a concentration-dependent manner, in the range (0.6-10 mM) known to inhibit ADPRT. benzamide 48-57 poly(ADP-ribose) polymerase 1 Homo sapiens 175-180 34885822-3 2021 In this study, a series of novel CRBN-recruiting HDAC PROTACs were designed and synthesized by linking hydroxamic acid and benzamide with lenalidomide, pomalidomide, and CC-220 through linkers of different lengths and types. benzamide 123-132 cereblon Homo sapiens 33-37 2143753-0 1990 Preparation and biological evaluation of 18F-labeled benzamide analogs as potential dopamine D2 receptor ligands. benzamide 53-62 dopamine receptor D2 Homo sapiens 84-104 2143753-1 1990 Three 18F-labeled benzamide derivatives were prepared and evaluated as potential ligands to study the dopamine D2 receptor phenomenon. benzamide 18-27 dopamine receptor D2 Homo sapiens 102-122 34894610-8 2022 Among the tested compounds 7a with benzamide moiety was the most potent dual DOR/KOR agonist. benzamide 35-44 opioid receptor kappa 1 Homo sapiens 81-84 34729902-0 2021 Mechanistic insights into the selective dual BET and PLK1 inhibitory activity of a novel benzamide compound in castration-resistant prostate cancer. benzamide 89-98 delta/notch like EGF repeat containing Homo sapiens 45-48 34729902-0 2021 Mechanistic insights into the selective dual BET and PLK1 inhibitory activity of a novel benzamide compound in castration-resistant prostate cancer. benzamide 89-98 polo like kinase 1 Homo sapiens 53-57 34885822-3 2021 In this study, a series of novel CRBN-recruiting HDAC PROTACs were designed and synthesized by linking hydroxamic acid and benzamide with lenalidomide, pomalidomide, and CC-220 through linkers of different lengths and types. benzamide 123-132 histone deacetylase 9 Homo sapiens 49-53 34478925-6 2021 Accordingly, in this paper, we have developed a reliable virtual screening process, combining different ligand- and structure-based methods, to identify novel benzamide-based analogs with potential HDAC1 inhibitory activity. benzamide 159-168 histone deacetylase 1 Homo sapiens 198-203 34478925-7 2021 For this purpose, a focused library of 736,160 compounds from PubChem database was first compiled based on 80% structural similarity with four known benzamide-based HDAC1 inhibitors, Mocetinostat, Entinostat, Tacedinaline, and Chidamide. benzamide 149-158 histone deacetylase 1 Homo sapiens 165-170 34428714-2 2021 Delightfully, benzylamine derivatives (14-27) exhibited higher ATX inhibitory potency with IC50 value ranging from 1.72 to 497 nM superior to benzamide analogues (8-13). benzamide 142-151 ectonucleotide pyrophosphatase/phosphodiesterase 2 Homo sapiens 63-66 34478925-13 2021 In summary, the presented computational approach can provide a set of guidelines for the further development of improved benzamide-based derivatives targeting HDAC1 isoform. benzamide 121-130 histone deacetylase 1 Homo sapiens 159-164 34314075-0 2021 Cf-02, a novel benzamide-linked small molecule, blunts NF-kappaB activation and NLRP3 inflammasome assembly and improves acute onset of accelerated and severe lupus nephritis in mice. benzamide 15-24 nuclear factor of kappa light polypeptide gene enhancer in B cells 1, p105 Mus musculus 55-64 34120025-0 2021 Synthesis, biological evaluation, and molecular docking analysis of novel linker-less benzamide based potent and selective HDAC3 inhibitors. benzamide 86-95 histone deacetylase 3 Mus musculus 123-128 34314075-0 2021 Cf-02, a novel benzamide-linked small molecule, blunts NF-kappaB activation and NLRP3 inflammasome assembly and improves acute onset of accelerated and severe lupus nephritis in mice. benzamide 15-24 NLR family, pyrin domain containing 3 Mus musculus 80-85 34314075-1 2021 In the present study, acute onset of severe lupus nephritis was successfully treated in mice using a new, benzamide-linked, small molecule that targets immune modulation and the NLRP3 inflammasome. benzamide 106-115 NLR family, pyrin domain containing 3 Mus musculus 178-183 35325883-3 2022 To gain specific targeting properties, NCs, XT5 molecules (a benzamide derivative) which shows high affinity properties against protease-activated receptor-1 (PAR1), that overexpressed in myeloma cancer cells, was used. benzamide 61-70 coagulation factor II thrombin receptor Homo sapiens 128-157 34165688-0 2022 New benzamide derivatives and their nicotinamide/cinnamamide analogs as cholinesterase inhibitors. benzamide 4-13 butyrylcholinesterase Homo sapiens 72-86 34165688-1 2022 In this study, a total of 18 new benzamide/ nicotinamide/ cinnamamide derivative compounds were designed and synthesized for the first time (except B1 and B5) by conventional and microwave irradiation methods. benzamide 33-42 immunoglobulin kappa variable 7-3 (pseudogene) Homo sapiens 148-157 35598794-0 2022 Synthesis and biological evaluation of new series of benzamide derivatives containing urea moiety as sEH inhibitors. benzamide 53-62 epoxide hydrolase 2 Homo sapiens 101-104 35483594-0 2022 In silico, synthesis and anticancer evaluation of benzamide tryptamine derivatives as novel eEF2K inhibitors. benzamide 50-59 eukaryotic elongation factor 2 kinase Homo sapiens 92-97 35325883-3 2022 To gain specific targeting properties, NCs, XT5 molecules (a benzamide derivative) which shows high affinity properties against protease-activated receptor-1 (PAR1), that overexpressed in myeloma cancer cells, was used. benzamide 61-70 coagulation factor II thrombin receptor Homo sapiens 159-163 35337122-0 2022 Development and Biological Evaluation of the First Highly Potent and Specific Benzamide-Based Radiotracer (18F)BA3 for Imaging of Histone Deacetylases 1 and 2 in Brain. benzamide 78-87 histone deacetylase 1 Homo sapiens 130-158 35450381-0 2022 Design, Synthesis, and Evaluation of PD-1/PD-L1 Antagonists Bearing a Benzamide Scaffold. benzamide 70-79 CD274 molecule Sus scrofa 42-47 35450381-3 2022 In this work, a series of novel benzamide derivatives were designed, synthesized, and evaluated to find effective inhibitors of the PD-1/PD-L1 interaction. benzamide 32-41 CD274 molecule Sus scrofa 137-142 35337122-3 2022 The aim of this work is the development of a novel 18F-labelled HDAC1/2-specific inhibitor with a benzamide-based zinc-binding group to visualize these enzymes in brain tumours by positron emission tomography (PET). benzamide 98-107 histone deacetylase 1 Homo sapiens 64-71 2529540-2 1989 On differentiation of the HL-60 cells into granulocytes induced by several inhibitors of poly(ADP-ribose) polymerase [NAD+ poly(adenosine diphosphate D-ribose)ADP-D-ribosyltransferase, EC 2.4.2.30] including benzamide, nicotinamide, coumarin, and 4-hydroxyquinazoline or dimethyl sulfoxide, some MYC loss was observed. benzamide 208-217 poly(ADP-ribose) polymerase 1 Homo sapiens 89-116 2531826-0 1989 [125]I-spectramide: a novel benzamide displaying potent and selective effects at the D2 dopamine receptor. benzamide 28-37 dopamine receptor D2 Rattus norvegicus 85-105 2555720-0 1989 The gastrointestinal prokinetic benzamide derivatives are agonists at the non-classical 5-HT receptor (5-HT4) positively coupled to adenylate cyclase in neurons. benzamide 32-41 5 hydroxytryptamine (serotonin) receptor 4 Mus musculus 103-108 2507758-3 1989 Benzamide (Bz), an inhibitor of adenosine diphosphoribosyl transferase (ADPRT), does not modify the lethal effect of UVC radiation in L5178Y-R cells, whereas it sensitizes L5178Y-S cells. benzamide 0-9 ADP-ribosyltransferase 1 Mus musculus 32-70 2507758-3 1989 Benzamide (Bz), an inhibitor of adenosine diphosphoribosyl transferase (ADPRT), does not modify the lethal effect of UVC radiation in L5178Y-R cells, whereas it sensitizes L5178Y-S cells. benzamide 0-9 ADP-ribosyltransferase 1 Mus musculus 72-77 2507758-3 1989 Benzamide (Bz), an inhibitor of adenosine diphosphoribosyl transferase (ADPRT), does not modify the lethal effect of UVC radiation in L5178Y-R cells, whereas it sensitizes L5178Y-S cells. benzamide 11-13 ADP-ribosyltransferase 1 Mus musculus 32-70 2507758-3 1989 Benzamide (Bz), an inhibitor of adenosine diphosphoribosyl transferase (ADPRT), does not modify the lethal effect of UVC radiation in L5178Y-R cells, whereas it sensitizes L5178Y-S cells. benzamide 11-13 ADP-ribosyltransferase 1 Mus musculus 72-77 2977324-1 1988 IBZM is one of several benzamide derivatives showing a high affinity for the CNS D-2 dopamine receptor. benzamide 23-32 dopamine receptor D2 Homo sapiens 81-102 2500442-11 1989 Drugs (such as benzamide and colchicine) that induce puffing of hsr omega, but not other heat shock loci, lead to large increases in omega 1. benzamide 15-24 Heat shock RNA omega Drosophila melanogaster 64-73 3148319-1 1988 The effect of treatment with benzamide, an inhibitor of adenosine diphosphate (ADP) ribosyl polymerase (ADPRP) was studied in cells of two strains of L5178Y (LY) murine lymphoma exposed to ionizing radiation. benzamide 29-38 poly (ADP-ribose) polymerase family, member 1 Mus musculus 104-109 3124848-1 1987 Structural analogues of benzamide (BA) containing a sulfur atom were tested for their ability to inhibit the enzyme poly(ADP-ribose)transferase (ADPRT) in cultured Chinese Hamster Ovary (CHO) cells. benzamide 24-33 poly [ADP-ribose] polymerase 1 Cricetulus griseus 116-143 3124848-1 1987 Structural analogues of benzamide (BA) containing a sulfur atom were tested for their ability to inhibit the enzyme poly(ADP-ribose)transferase (ADPRT) in cultured Chinese Hamster Ovary (CHO) cells. benzamide 24-33 poly [ADP-ribose] polymerase 1 Cricetulus griseus 145-150 3124848-1 1987 Structural analogues of benzamide (BA) containing a sulfur atom were tested for their ability to inhibit the enzyme poly(ADP-ribose)transferase (ADPRT) in cultured Chinese Hamster Ovary (CHO) cells. benzamide 35-37 poly [ADP-ribose] polymerase 1 Cricetulus griseus 116-143 3124848-1 1987 Structural analogues of benzamide (BA) containing a sulfur atom were tested for their ability to inhibit the enzyme poly(ADP-ribose)transferase (ADPRT) in cultured Chinese Hamster Ovary (CHO) cells. benzamide 35-37 poly [ADP-ribose] polymerase 1 Cricetulus griseus 145-150 3124848-5 1987 TCA, an isostere of BA, produced some inhibition of ADPRT, although its activity was markedly lower than that of the parental drug. benzamide 20-22 poly [ADP-ribose] polymerase 1 Cricetulus griseus 52-57 3742029-4 1986 Other benzamide derivatives were less active in inhibiting MAO-A and had but a negligible effect on dopamine- and 2-phenylethylamine deamination. benzamide 6-15 monoamine oxidase A Rattus norvegicus 59-64 2942307-1 1986 The effect of nicotinamide or benzamide, inhibitors of poly(ADP-ribose)polymerase activity, on X-ray and ultraviolet light induced killing of asynchronously dividing V79 Chinese hamster cells was to reduce the shoulder width of the survival curve; the rate of killing remaining unchanged and the yield of 8-azaguanine resistant mutants also remaining unaffected. benzamide 30-39 poly [ADP-ribose] polymerase 1 Cricetulus griseus 55-81 3132517-5 1987 The radiometric test procedure (CV 20-25%) is critically validated and kinetic properties of serum ADPRT have been studied, showing a competitive inhibition by nicotinamide, benzamide and 3-aminobenzamide. benzamide 174-183 poly(ADP-ribose) polymerase 1 Homo sapiens 99-104 3299396-2 1987 The substituted benzamide, sulpiride, a selective dopamine D-2 receptor antagonist, significantly increased the consumption of water and hypotonic saline at 30 mg/kg. benzamide 16-25 solute carrier family 3 member 1 Rattus norvegicus 59-62 3114030-1 1987 Previous studies have shown that benzamide and nicotinamide, two inhibitors of poly(ADP-ribose) polymerase, induce erythroid differentiation in Friend erythroleukemic cells. benzamide 33-42 poly(ADP-ribose) polymerase 1 Homo sapiens 79-106 4030988-3 1985 Internal standards were a new substituted benzamide (N-[(ethyl-1-pyrrolidinyl-2)methyl] methoxy-2-ethylsulphonyl-5-benzamide, DAN) for the sulpiride assay and sulpiride for the sultopride assay. benzamide 42-51 NBL1, DAN family BMP antagonist Homo sapiens 126-129 3088638-1 1986 BRL 20596 (N-(4-amino-5-chloro-2-methoxyphenyl)-1-phenylmethyl-4-piperidine-carbox amide) is a novel anilide related to clebopride (a gastric prokinetic benzamide) in which the sole change is reversal of the amide bond. benzamide 153-162 bromodomain containing 1 Homo sapiens 0-3 3761757-5 1986 In the D-2 receptor assay, the IC50 values of tiapride and sulpiride were 1/22.7 and 1/19.1 of those in the presence of 100 mM NaCl, respectively, suggesting that benzamide drug binds to the D-2 subtype with higher affinity in the presence of Na+ than in the control. benzamide 163-172 solute carrier family 3 member 1 Rattus norvegicus 7-10 3761757-5 1986 In the D-2 receptor assay, the IC50 values of tiapride and sulpiride were 1/22.7 and 1/19.1 of those in the presence of 100 mM NaCl, respectively, suggesting that benzamide drug binds to the D-2 subtype with higher affinity in the presence of Na+ than in the control. benzamide 163-172 solute carrier family 3 member 1 Rattus norvegicus 191-194 6616329-1 1983 While a first injection of the antidopaminergic benzamide drug, sulpiride, induced a large rise in plasma prolactin (PRL) levels in chronically cannulated adult male rats, a second injection given 2 h later was totally inactive although the pituitary content of the hormone was still 76% of the initial value. benzamide 48-57 prolactin Rattus norvegicus 106-115 6196785-4 1983 Benzamide (10 microM intracellular concentration), a specific inhibitor of poly(ADP-ribose) polymerase, prevented transformation in a cell cycle-specific manner, maximal prevention coinciding with early S phase, also characteristic of maximal susceptibility to transformation. benzamide 0-9 poly(ADP-ribose) polymerase 1 Homo sapiens 75-102 4026902-4 1985 The reversible and specific monoamine oxidase (MAO)-A inhibitor moclobemide, a benzamide, is therefore completely different from the classical irreversible MAO inhibitors of the hydrazine type and, as also confirmed in the clinical studies, does not have any hepatotoxic effect. benzamide 79-88 monoamine oxidase A Rattus norvegicus 28-53 4026902-4 1985 The reversible and specific monoamine oxidase (MAO)-A inhibitor moclobemide, a benzamide, is therefore completely different from the classical irreversible MAO inhibitors of the hydrazine type and, as also confirmed in the clinical studies, does not have any hepatotoxic effect. benzamide 79-88 monoamine oxidase A Rattus norvegicus 47-50 6388247-2 1984 Moclobemide (Ro 11-1163), a benzamide derivative, is a MAO-inhibitor which selectively and reversibly inhibits monoamine oxidase type A. benzamide 28-37 monoamine oxidase A Homo sapiens 111-135 6087814-1 1984 Rats fed a synthetic diet containing 0.25% benzamide, 0.1% phenobarbital, separately or in combination, for two weeks showed a significant augmentation in the activity of nuclear poly(ADP-ribose) polymerase as well as changes in various nuclear, microsomal and cytosolic liver enzymes involved in the metabolism of xenobiotics. benzamide 43-52 poly (ADP-ribose) polymerase 1 Rattus norvegicus 179-206 6616329-1 1983 While a first injection of the antidopaminergic benzamide drug, sulpiride, induced a large rise in plasma prolactin (PRL) levels in chronically cannulated adult male rats, a second injection given 2 h later was totally inactive although the pituitary content of the hormone was still 76% of the initial value. benzamide 48-57 prolactin Rattus norvegicus 117-120 1147723-2 1975 Four structuraly related benzamide derivative (1211, 1265, 1308 and 1347) also stimutated the ileum, 1211 being the most active, and 1347 the least active, and resembled Mcp with regard to the responses to Ac, transmural stimulation and histamine. benzamide 25-34 membrane cofactor protein Cavia porcellus 171-174 6855475-2 1983 Nevertheless, the IC50 values for the inhibition of 3H-spiperone binding by the seven substituted benzamide drugs was significantly correlated with their high potency to stimulate rat PRL secretion in vivo. benzamide 98-107 prolactin Rattus norvegicus 184-187 6855475-5 1983 This data suggests that blockade of different subgroups of dopamine receptors in the anterior pituitary gland labeled by 3H-spiperone may be responsible for the in vivo stimulation of PRL secretion by the benzamide and non-benzamide neuroleptic drugs. benzamide 205-214 prolactin Rattus norvegicus 184-187 7256107-1 1981 The authors report results attained by means of a replaced benzamide, thiapride, in the treatment of 21 subjects showing involuntary movements of extra-pyramidal origin and more exactly: extra-pyramidal syndromes due to drugs (3), idiopathic dyscinesias (8), choreas (6), dystonias (3), essential tremor (1). benzamide 59-68 dopamine receptor D3 Homo sapiens 287-307 6884428-2 1983 The inhibition by (-)-NCA was reversible and antagonized by the benzamide neuroleptic S-sulpiride. benzamide 64-73 CEA cell adhesion molecule 6 Homo sapiens 22-25 6827920-0 1983 Effect of a novel benzamide, YM-09151-2, on rat serum prolactin levels. benzamide 18-27 prolactin Rattus norvegicus 54-63 6827920-4 1983 This benzamide was also a potent blocker of DA-induced inhibition of prolactin release in vitro and was very effective in displacing 3H-spiperone from bovine pituitary membranes: IC50, 1.04nM. benzamide 5-14 prolactin Bos taurus 69-78 6307677-1 1983 Benzamide and 3-aminobenzamide, inhibitors of poly(ADP-ribose) polymerase, synergistically enhanced the frequencies of unscheduled DNA synthesis and sister chromatid exchanges in Chinese hamster ovary (CHO) cells treated with N-methyl-N"-nitro-N-nitrosoguanidine (MNNG). benzamide 0-9 poly [ADP-ribose] polymerase 1 Cricetulus griseus 46-73 33987736-0 2021 Identification of benzamide inhibitors of histone deacetylase 1 from Babesia and Theileria species via high-throughput virtual screening and molecular dynamics simulations. benzamide 18-27 histone deacetylase 1 Homo sapiens 42-63 33987736-6 2021 We have herein focused on the class I HDAC enzyme, HDAC1, of the Babesia and Theileria species to discover potential benzamide inhibitors by following a streamlined workflow of computer-aided drug design methodology. benzamide 117-126 histone deacetylase 9 Homo sapiens 38-42 33577290-0 2021 PT3: A Novel Benzamide Class Histone Deacetylase 3 Inhibitor Improves Learning and Memory in Novel Object Recognition Mouse Model. benzamide 13-22 histone deacetylase 3 Mus musculus 29-50 33858315-0 2022 Evaluation of Benzamide-chalcone Derivatives as EGFR/CDK2 inhibitor: Synthesis, in-vitro Inhibition, and Molecular Modeling Studies. benzamide 14-23 epidermal growth factor receptor Homo sapiens 48-52 33858315-0 2022 Evaluation of Benzamide-chalcone Derivatives as EGFR/CDK2 inhibitor: Synthesis, in-vitro Inhibition, and Molecular Modeling Studies. benzamide 14-23 cyclin dependent kinase 2 Homo sapiens 53-57 33858315-17 2022 CONCLUSION: These benzamide-substituted chalcone derivatives will be useful as lead molecules for the further development of newer inhibitors of EGFR and/or CDK2 kinases. benzamide 18-27 epidermal growth factor receptor Homo sapiens 145-149 33858315-17 2022 CONCLUSION: These benzamide-substituted chalcone derivatives will be useful as lead molecules for the further development of newer inhibitors of EGFR and/or CDK2 kinases. benzamide 18-27 cyclin dependent kinase 2 Homo sapiens 157-161 33987736-6 2021 We have herein focused on the class I HDAC enzyme, HDAC1, of the Babesia and Theileria species to discover potential benzamide inhibitors by following a streamlined workflow of computer-aided drug design methodology. benzamide 117-126 histone deacetylase 1 Homo sapiens 51-56 33987736-7 2021 Molecular docking and molecular dynamics simulations revealed that benzamide derivatives stably interacted with the HDAC1 active site in both parasites as hypothesized. benzamide 67-76 histone deacetylase 1 Homo sapiens 116-121 33885193-2 2021 The methodology furnished a set of benzamide model compounds, including the two poly (ADP-ribose) polymerase (PARP) inhibitors niraparib and veliparib, in moderate to excellent radiochemical yields. benzamide 35-44 poly(ADP-ribose) polymerase 1 Homo sapiens 80-108 33885193-2 2021 The methodology furnished a set of benzamide model compounds, including the two poly (ADP-ribose) polymerase (PARP) inhibitors niraparib and veliparib, in moderate to excellent radiochemical yields. benzamide 35-44 poly(ADP-ribose) polymerase 1 Homo sapiens 110-114 33671108-0 2021 The Novel Benzamide Derivative, VKNG-2, Restores the Efficacy of Chemotherapeutic Drugs in Colon Cancer Cell Lines by Inhibiting the ABCG2 Transporter. benzamide 10-19 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 133-138 33671108-3 2021 In this study, we determined the efficacy of the novel benzamide derivative, VKNG-2, to overcome MDR due to the overexpression of the ABCG2 transporter in the colon cancer cell line, S1-M1-80. benzamide 55-64 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 134-139 33339666-0 2021 Synthesis, crystal structure and Hirshfeld Surface analysis of benzamide derivatives of thiourea as potent inhibitors of alpha-glucosidase in-vitro. benzamide 63-72 sucrase isomaltase (alpha-glucosidase) Mus musculus 121-138 33339666-1 2021 Benzamide based structural analogues 1-15 were synthesized, and evaluated for alpha-glucosidase inhibition activity in vitro for the first time. benzamide 0-9 sucrase isomaltase (alpha-glucosidase) Mus musculus 78-95 32416556-0 2020 Corrigendum to "Optimization of the benzamide fragment targeting the S2" site leads to potent dipeptidyl Peptidase-IV inhibitors" [Bioorg. benzamide 36-45 dipeptidyl peptidase 4 Homo sapiens 94-117 33335670-0 2020 Discovery of Highly Selective and Potent HDAC3 Inhibitors Based on a 2-Substituted Benzamide Zinc Binding Group. benzamide 83-92 histone deacetylase 3 Homo sapiens 41-46 33488256-0 2020 Synthesis and pharmacological effects of novel benzenesulfonamides carrying benzamide moiety as carbonic anhydrase and acetylcholinesterase inhibitors. benzamide 76-85 acetylcholinesterase (Cartwright blood group) Homo sapiens 119-139 32653824-1 2020 Though it has been demonstrated that Chidamide (CS055/HBI-8000), a novel benzamide class of histone deacetylase (HDAC) subtype-selectively inhibitor, reveals better anticancer effect in acute leukemia, but it remains unknown about the precise mechanism of Chidamide-induced acute leukemia cell apoptosis due to the lack of in situ molecular changes information. benzamide 73-82 histone deacetylase 9 Homo sapiens 92-111 32653824-1 2020 Though it has been demonstrated that Chidamide (CS055/HBI-8000), a novel benzamide class of histone deacetylase (HDAC) subtype-selectively inhibitor, reveals better anticancer effect in acute leukemia, but it remains unknown about the precise mechanism of Chidamide-induced acute leukemia cell apoptosis due to the lack of in situ molecular changes information. benzamide 73-82 histone deacetylase 9 Homo sapiens 113-117 33102692-0 2020 FOXA1 Regulation Turns Benzamide HDACi Treatment Effect-Specific in BC, Promoting NIS Gene-Mediated Targeted Radioiodine Therapy. benzamide 23-32 forkhead box A1 Homo sapiens 0-5 32325365-0 2020 Purine/purine isoster based scaffolds as new derivatives of benzamide class of HDAC inhibitors. benzamide 60-69 histone deacetylase 9 Homo sapiens 79-83 31963723-0 2020 Profiling the Structural Determinants of Aryl Benzamide Derivatives as Negative Allosteric Modulators of mGluR5 by In Silico Study. benzamide 41-55 glutamate receptor, ionotropic, kainate 1 Mus musculus 105-111 31910010-3 2020 Structure-activity relationship-driven expansion of a fragment hit led to discovery of dual MNK1 and MNK2 inhibitors based on a novel pyridine-benzamide scaffold. benzamide 134-152 MAPK interacting serine/threonine kinase 1 Homo sapiens 92-96 31910010-3 2020 Structure-activity relationship-driven expansion of a fragment hit led to discovery of dual MNK1 and MNK2 inhibitors based on a novel pyridine-benzamide scaffold. benzamide 134-152 MAPK interacting serine/threonine kinase 2 Homo sapiens 101-105 31963723-2 2020 At present, to explore the structural features of 106 newly synthesized aryl benzamide series molecules as mGluR5 NAMs, a set of ligand-based three-dimensional quantitative structure-activity relationship (3D-QSAR) analyses were firstly carried out applying comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA) methods. benzamide 72-86 glutamate receptor, ionotropic, kainate 1 Mus musculus 107-113 31963723-5 2020 Moreover, we found that aryl benzamide series molecules bind as mGluR5 NAMs at Site 1, which consists of amino acids Pro655, Tyr659, Ile625, Ile651, Ile944, Ser658, Ser654, Ser969, Ser965, Ala970, Ala973, Trp945, Phe948, Pro903, Asn907, Val966, Leu904, and Met962. benzamide 24-38 glutamate receptor, ionotropic, kainate 1 Mus musculus 64-70 31963723-5 2020 Moreover, we found that aryl benzamide series molecules bind as mGluR5 NAMs at Site 1, which consists of amino acids Pro655, Tyr659, Ile625, Ile651, Ile944, Ser658, Ser654, Ser969, Ser965, Ala970, Ala973, Trp945, Phe948, Pro903, Asn907, Val966, Leu904, and Met962. benzamide 24-38 interferon epsilon Homo sapiens 117-123 31640932-0 2020 Optimization of the benzamide fragment targeting the S2" site leads to potent dipeptidyl peptidase-IV inhibitors. benzamide 20-29 dipeptidyl peptidase 4 Homo sapiens 78-101 31670334-0 2019 Cp*CoIII-catalyzed formal [4+2] cycloaddition of benzamides to afford quinazolinone derivatives. benzamide 49-59 mitochondrially encoded cytochrome c oxidase III Homo sapiens 3-8 31169043-0 2019 Synthesis and characterisation of a new benzamide-containing nitrobenzoxadiazole as a GSTP1-1 inhibitor endowed with high stability to metabolic hydrolysis. benzamide 40-49 glutathione S-transferase pi 1 Homo sapiens 86-93 31670334-1 2019 A Cp*CoIII-catalyzed arene C-H bond amidation/annulation of benzamides was developed to afford quinazolinone derivatives in one-pot with high yields and broad substrate scope. benzamide 60-70 mitochondrially encoded cytochrome c oxidase III Homo sapiens 5-10 31378596-0 2019 Microwave-Assisted Organic Synthesis, structure-activity relationship, kinetics and molecular docking studies of non-cytotoxic benzamide derivatives as selective butyrylcholinesterase inhibitors. benzamide 127-136 butyrylcholinesterase Homo sapiens 162-183 31439379-0 2019 Design, synthesis and biological evaluation of benzamide derivatives as novel NTCP inhibitors that induce apoptosis in HepG2 cells. benzamide 47-56 solute carrier family 10 member 1 Homo sapiens 78-82 31933782-1 2019 OBJECTIVE: To study the function and mechanism of combined PARP-1 and BRCA genes in regulating the radiosensitivity of breast cancer cells by poly ADP-ribose polymerase-1 (PARP-1) inhibitor 3-amion benzamide (3-AB) onBRCA mutant and non-mutant breast cancer cells. benzamide 190-207 poly(ADP-ribose) polymerase 1 Homo sapiens 59-65 31933782-1 2019 OBJECTIVE: To study the function and mechanism of combined PARP-1 and BRCA genes in regulating the radiosensitivity of breast cancer cells by poly ADP-ribose polymerase-1 (PARP-1) inhibitor 3-amion benzamide (3-AB) onBRCA mutant and non-mutant breast cancer cells. benzamide 190-207 BRCA1 DNA repair associated Homo sapiens 70-74 31933782-1 2019 OBJECTIVE: To study the function and mechanism of combined PARP-1 and BRCA genes in regulating the radiosensitivity of breast cancer cells by poly ADP-ribose polymerase-1 (PARP-1) inhibitor 3-amion benzamide (3-AB) onBRCA mutant and non-mutant breast cancer cells. benzamide 190-207 poly(ADP-ribose) polymerase 1 Homo sapiens 142-170 31933782-1 2019 OBJECTIVE: To study the function and mechanism of combined PARP-1 and BRCA genes in regulating the radiosensitivity of breast cancer cells by poly ADP-ribose polymerase-1 (PARP-1) inhibitor 3-amion benzamide (3-AB) onBRCA mutant and non-mutant breast cancer cells. benzamide 190-207 poly(ADP-ribose) polymerase 1 Homo sapiens 172-178 31933782-1 2019 OBJECTIVE: To study the function and mechanism of combined PARP-1 and BRCA genes in regulating the radiosensitivity of breast cancer cells by poly ADP-ribose polymerase-1 (PARP-1) inhibitor 3-amion benzamide (3-AB) onBRCA mutant and non-mutant breast cancer cells. benzamide 209-213 poly(ADP-ribose) polymerase 1 Homo sapiens 59-65 31933782-1 2019 OBJECTIVE: To study the function and mechanism of combined PARP-1 and BRCA genes in regulating the radiosensitivity of breast cancer cells by poly ADP-ribose polymerase-1 (PARP-1) inhibitor 3-amion benzamide (3-AB) onBRCA mutant and non-mutant breast cancer cells. benzamide 209-213 BRCA1 DNA repair associated Homo sapiens 70-74 31933782-1 2019 OBJECTIVE: To study the function and mechanism of combined PARP-1 and BRCA genes in regulating the radiosensitivity of breast cancer cells by poly ADP-ribose polymerase-1 (PARP-1) inhibitor 3-amion benzamide (3-AB) onBRCA mutant and non-mutant breast cancer cells. benzamide 209-213 poly(ADP-ribose) polymerase 1 Homo sapiens 142-170 31933782-1 2019 OBJECTIVE: To study the function and mechanism of combined PARP-1 and BRCA genes in regulating the radiosensitivity of breast cancer cells by poly ADP-ribose polymerase-1 (PARP-1) inhibitor 3-amion benzamide (3-AB) onBRCA mutant and non-mutant breast cancer cells. benzamide 209-213 poly(ADP-ribose) polymerase 1 Homo sapiens 172-178 31378596-1 2019 A series of benzamide derivatives 1-12 with various functional groups (-H, -Br, -F, -OCH3, -OC2H5, and -NO2) was synthesized using an economic, and facile Microwave-Assisted Organic Synthesis, and evaluated for acetylcholinesterase (ACHE) and butyrylcholinesterase (BCHE) activity in vitro. benzamide 12-21 acetylcholinesterase (Cartwright blood group) Homo sapiens 211-231 31327679-1 2019 For the purpose of synthesizing drug candidates with desirable bioactivity, a class of benzoyl amide containing nitrogen heterocyclic ring derivatives targeting VEGFR-2 was designed and screened out using Discovery Studio. benzamide 87-100 kinase insert domain receptor Homo sapiens 161-168 31378596-1 2019 A series of benzamide derivatives 1-12 with various functional groups (-H, -Br, -F, -OCH3, -OC2H5, and -NO2) was synthesized using an economic, and facile Microwave-Assisted Organic Synthesis, and evaluated for acetylcholinesterase (ACHE) and butyrylcholinesterase (BCHE) activity in vitro. benzamide 12-21 acetylcholinesterase (Cartwright blood group) Homo sapiens 233-237 31378596-1 2019 A series of benzamide derivatives 1-12 with various functional groups (-H, -Br, -F, -OCH3, -OC2H5, and -NO2) was synthesized using an economic, and facile Microwave-Assisted Organic Synthesis, and evaluated for acetylcholinesterase (ACHE) and butyrylcholinesterase (BCHE) activity in vitro. benzamide 12-21 butyrylcholinesterase Homo sapiens 243-264 31378596-1 2019 A series of benzamide derivatives 1-12 with various functional groups (-H, -Br, -F, -OCH3, -OC2H5, and -NO2) was synthesized using an economic, and facile Microwave-Assisted Organic Synthesis, and evaluated for acetylcholinesterase (ACHE) and butyrylcholinesterase (BCHE) activity in vitro. benzamide 12-21 butyrylcholinesterase Homo sapiens 266-270 30179749-0 2018 HDAC3 is a potential validated target for cancer: An overview on the benzamide-based selective HDAC3 inhibitors through comparative SAR/QSAR/QAAR approaches. benzamide 69-78 histone deacetylase 3 Homo sapiens 0-5 31327679-0 2019 Design, synthesis, biological evaluation of benzoyl amide derivatives containing nitrogen heterocyclic ring as potential VEGFR-2 inhibitors. benzamide 44-57 kinase insert domain receptor Homo sapiens 121-128 30826710-2 2019 In the present study, a series of heteroaryl benzamide derivatives were selected as potent inhibitors against InhA, and their binding properties with InhA were investigated at atomic and electronic levels by ab initio molecular simulations based on protein-ligand docking, classical molecular mechanics optimizations and ab initio fragment molecular orbital (FMO) calculations. benzamide 45-54 inhibin subunit alpha Homo sapiens 110-114 30826710-2 2019 In the present study, a series of heteroaryl benzamide derivatives were selected as potent inhibitors against InhA, and their binding properties with InhA were investigated at atomic and electronic levels by ab initio molecular simulations based on protein-ligand docking, classical molecular mechanics optimizations and ab initio fragment molecular orbital (FMO) calculations. benzamide 45-54 inhibin subunit alpha Homo sapiens 150-154 30826710-4 2019 These findings provide informative structural concepts for designing novel heteroaryl benzamide derivatives with higher binding affinity to InhA. benzamide 86-95 inhibin subunit alpha Homo sapiens 140-144 30702760-1 2019 A series of benzamide derivatives possessing potent dopamine D2 , serotonin 5-HT1A , and 5-HT2A receptor properties were synthesized and evaluated as potential antipsychotics. benzamide 12-21 5-hydroxytryptamine receptor 1A Homo sapiens 76-82 30702760-1 2019 A series of benzamide derivatives possessing potent dopamine D2 , serotonin 5-HT1A , and 5-HT2A receptor properties were synthesized and evaluated as potential antipsychotics. benzamide 12-21 5-hydroxytryptamine receptor 2A Homo sapiens 91-95 30735902-9 2019 In this review, detail chemico-biological and structural information of HDAC3 in memory and learning functions and benzamide-based HDAC3 inhibitors has been focussed. benzamide 115-124 histone deacetylase 3 Homo sapiens 131-136 30735902-10 2019 This may help to achieve a deep insight so that potent and selective benzamide-based HDAC3 inhibitors may be designed in future to combat memory and learning-related dysfunctions. benzamide 69-78 histone deacetylase 3 Homo sapiens 85-90 30354009-9 2019 We proposed various chemical scaffolds including benzamide, carboxamide, and methyl benzimidazole targeting Akt2 and thus may act as potential leads for the further development of new anticancer agents. benzamide 49-58 AKT serine/threonine kinase 2 Homo sapiens 108-112 29166796-0 2018 Structure-activity relationship investigation of benzamide and picolinamide derivatives containing dimethylamine side chain as acetylcholinesterase inhibitors. benzamide 49-58 acetylcholinesterase (Cartwright blood group) Homo sapiens 127-147 30351001-3 2018 In this study, inspired by the conclusion that ligand-induced "Phe199 shift" effect is the structural basis of Grp94-selective inhibition, a series of novel Grp94 selective inhibitors incorporating "benzamide" moiety were developed, among which compound 54 manifested the most potent Grp94 inhibitory activity with an IC50 value of 2 nM and over 1000-fold selectivity to Grp94 against Hsp90alpha. benzamide 199-208 heat shock protein 90, beta (Grp94), member 1 Mus musculus 111-116 30351001-3 2018 In this study, inspired by the conclusion that ligand-induced "Phe199 shift" effect is the structural basis of Grp94-selective inhibition, a series of novel Grp94 selective inhibitors incorporating "benzamide" moiety were developed, among which compound 54 manifested the most potent Grp94 inhibitory activity with an IC50 value of 2 nM and over 1000-fold selectivity to Grp94 against Hsp90alpha. benzamide 199-208 heat shock protein 90, beta (Grp94), member 1 Mus musculus 157-162 30351001-3 2018 In this study, inspired by the conclusion that ligand-induced "Phe199 shift" effect is the structural basis of Grp94-selective inhibition, a series of novel Grp94 selective inhibitors incorporating "benzamide" moiety were developed, among which compound 54 manifested the most potent Grp94 inhibitory activity with an IC50 value of 2 nM and over 1000-fold selectivity to Grp94 against Hsp90alpha. benzamide 199-208 heat shock protein 90, beta (Grp94), member 1 Mus musculus 157-162 30351001-3 2018 In this study, inspired by the conclusion that ligand-induced "Phe199 shift" effect is the structural basis of Grp94-selective inhibition, a series of novel Grp94 selective inhibitors incorporating "benzamide" moiety were developed, among which compound 54 manifested the most potent Grp94 inhibitory activity with an IC50 value of 2 nM and over 1000-fold selectivity to Grp94 against Hsp90alpha. benzamide 199-208 heat shock protein 90, beta (Grp94), member 1 Mus musculus 157-162 29935282-0 2018 A novel benzamide derivative protects ligature-induced alveolar bone erosion by inhibiting NFATc1-mediated osteoclastogenesis. benzamide 8-17 nuclear factor of activated T cells, cytoplasmic, calcineurin dependent 1 Mus musculus 91-97 30179749-8 2018 However, the importance of spiro hydrophobic cap group, as well as electron withdrawing fluorine group at the benzamide scaffold, should be well-accounted for retaining higher HDAC3 selectivity over HDAC1. benzamide 110-119 histone deacetylase 1 Homo sapiens 199-204 30179749-10 2018 This detailed structural exploration will surely unveil a new vista of designing highly potent and selective benzamide-based HDAC3 inhibitors that may be a crucial weapon to battle against a variety of cancers. benzamide 109-118 histone deacetylase 3 Homo sapiens 125-130 31330099-4 2019 Hydroxamic-acid-based inhibitors of HDACs 1-3, reported to have fast-on/fast-off binding kinetics, induce increased expression of PGRN in human neuronal models, while the benzamide class of slow-binding HDAC inhibitors does not produce this effect. benzamide 171-180 histone deacetylase 1 Homo sapiens 36-45 31330099-4 2019 Hydroxamic-acid-based inhibitors of HDACs 1-3, reported to have fast-on/fast-off binding kinetics, induce increased expression of PGRN in human neuronal models, while the benzamide class of slow-binding HDAC inhibitors does not produce this effect. benzamide 171-180 histone deacetylase 9 Homo sapiens 36-40 30044204-1 2019 The work presented here explores the structural and physicochemical features important for benzamide-based HDAC3 inhibitors to get an idea about the design aspect of potential inhibitors. benzamide 91-100 histone deacetylase 3 Homo sapiens 107-112 30044204-2 2019 A number of molecular modeling studies (3D-QSAR CoMFA and CoMSIA, Bayesian classification modeling) were performed on 113 diverse set of benzamide-based HDAC3 inhibitors. benzamide 137-146 histone deacetylase 3 Homo sapiens 153-158 30179749-0 2018 HDAC3 is a potential validated target for cancer: An overview on the benzamide-based selective HDAC3 inhibitors through comparative SAR/QSAR/QAAR approaches. benzamide 69-78 histone deacetylase 3 Homo sapiens 95-100 30179749-0 2018 HDAC3 is a potential validated target for cancer: An overview on the benzamide-based selective HDAC3 inhibitors through comparative SAR/QSAR/QAAR approaches. benzamide 69-78 sarcosine dehydrogenase Homo sapiens 132-135 30179749-4 2018 Nowadays, compounds comprising benzamide functionality as zinc binding group (ZBG) have been emerged out to be highly effective and selective HDAC3 inhibitors. benzamide 31-40 histone deacetylase 3 Homo sapiens 142-147 30179749-5 2018 In this article, QSAR and QAAR studies have been conducted on diverse benzamide-derived HDAC3 inhibitors as the first initiative to explore the designing strategies of higher active and selective HDAC3 inhibitors over HDAC1 and HDAC2. benzamide 70-79 histone deacetylase 3 Homo sapiens 88-93 30179749-5 2018 In this article, QSAR and QAAR studies have been conducted on diverse benzamide-derived HDAC3 inhibitors as the first initiative to explore the designing strategies of higher active and selective HDAC3 inhibitors over HDAC1 and HDAC2. benzamide 70-79 histone deacetylase 3 Homo sapiens 196-201 30179749-5 2018 In this article, QSAR and QAAR studies have been conducted on diverse benzamide-derived HDAC3 inhibitors as the first initiative to explore the designing strategies of higher active and selective HDAC3 inhibitors over HDAC1 and HDAC2. benzamide 70-79 histone deacetylase 1 Homo sapiens 218-223 30179749-5 2018 In this article, QSAR and QAAR studies have been conducted on diverse benzamide-derived HDAC3 inhibitors as the first initiative to explore the designing strategies of higher active and selective HDAC3 inhibitors over HDAC1 and HDAC2. benzamide 70-79 histone deacetylase 2 Homo sapiens 228-233 30179749-7 2018 QAAR models reflect that modification/substitution at the benzamide scaffold should be optimized in such a way so that these molecules possess lower steric bulk along with nonpolar features for achieving higher HDAC3 selectivity over HDAC1 and HDAC2. benzamide 58-67 histone deacetylase 3 Homo sapiens 211-216 30179749-7 2018 QAAR models reflect that modification/substitution at the benzamide scaffold should be optimized in such a way so that these molecules possess lower steric bulk along with nonpolar features for achieving higher HDAC3 selectivity over HDAC1 and HDAC2. benzamide 58-67 histone deacetylase 1 Homo sapiens 234-239 30179749-7 2018 QAAR models reflect that modification/substitution at the benzamide scaffold should be optimized in such a way so that these molecules possess lower steric bulk along with nonpolar features for achieving higher HDAC3 selectivity over HDAC1 and HDAC2. benzamide 58-67 histone deacetylase 2 Homo sapiens 244-249 30179749-8 2018 However, the importance of spiro hydrophobic cap group, as well as electron withdrawing fluorine group at the benzamide scaffold, should be well-accounted for retaining higher HDAC3 selectivity over HDAC1. benzamide 110-119 histone deacetylase 3 Homo sapiens 176-181 29853338-4 2018 In this article, 24 benzamide derivatives were designed, synthesized and investigated for the inhibition activity against CDK2. benzamide 20-29 cyclin dependent kinase 2 Homo sapiens 122-126 29301237-0 2017 Synthesis and Smo Activity of Some Novel Benzamide Derivatives. benzamide 41-50 smoothened, frizzled class receptor Homo sapiens 14-17 29862624-1 2018 By making use of a dual-chelation-assisted strategy, a completely regiocontrolled oxidative C-H/C-H cross-coupling reaction between an N-acylaniline and a benzamide has been accomplished for the first time. benzamide 155-164 churchill domain containing 1 Homo sapiens 92-99 29953251-6 2018 The hydrophobic aryl cap function is important for HDAC8 inhibition whereas benzamide moiety shows a negative impact on HDAC8 inhibition. benzamide 76-85 histone deacetylase 8 Homo sapiens 120-125 29206502-6 2017 In conclusion, it is observed that the lead compounds #2 and #5 possessed inhibitory activity on the hGSTP1-1 by binding to the H-site as a substrate in which the para position of the phenyl ring of the benzamide moiety on the benzothiazole ring is important. benzamide 203-212 glutathione S-transferase pi 1 Homo sapiens 101-109 28916341-0 2017 Design, synthesis and biological evaluation of benzamide and phenyltetrazole derivatives with amide and urea linkers as BCRP inhibitors. benzamide 47-56 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 120-124 28916341-3 2017 A series of 31 benzamide and phenyltetrazole derivatives with amide and urea linkers has been synthesized to serve as potential BCRP inhibitors in order to overcome BCRP-mediated MDR. benzamide 15-24 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 128-132 28916341-3 2017 A series of 31 benzamide and phenyltetrazole derivatives with amide and urea linkers has been synthesized to serve as potential BCRP inhibitors in order to overcome BCRP-mediated MDR. benzamide 15-24 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 165-169 28756263-6 2017 Among them, compounds 7i, w, y with Cl, CN or NO2 groups at the 4-position of the benzamide scaffold showed excellent affinity for S1R (Ki = 1.2-3.6 nM), selectivity for S2R (Ki up to 1400 nM) and high selectivity index (IC50(SY5Y)/Ki(S1R) ratio from 28 000 to 83 000). benzamide 82-91 transmembrane BAX inhibitor motif containing 4 Homo sapiens 131-134 28807572-2 2017 Further derivatization of the prototype dual orexin receptor 1/2 antagonist lead (1) by installing a (S)-methyl group into the ethyl linker moiety between the pyrazole ring and benzamide resulted in an increase of the antagonist potency against orexin receptor 1/2 receptors. benzamide 177-186 hypocretin receptor 1 Homo sapiens 45-62 28807572-2 2017 Further derivatization of the prototype dual orexin receptor 1/2 antagonist lead (1) by installing a (S)-methyl group into the ethyl linker moiety between the pyrazole ring and benzamide resulted in an increase of the antagonist potency against orexin receptor 1/2 receptors. benzamide 177-186 hypocretin receptor 1 Homo sapiens 45-64 29103972-1 2017 Optimization of benzamide PPARdelta modulator 1 led to (E)-6-(2-((4-(furan-2-yl)-N-methylbenzamido)methyl)phenoxy)-4-methylhex-4-enoic acid (18), a potent selective PPARdelta modulator with significantly improved exposure in multiple species following oral administration. benzamide 16-25 peroxisome proliferator activated receptor delta Homo sapiens 26-35 29103972-1 2017 Optimization of benzamide PPARdelta modulator 1 led to (E)-6-(2-((4-(furan-2-yl)-N-methylbenzamido)methyl)phenoxy)-4-methylhex-4-enoic acid (18), a potent selective PPARdelta modulator with significantly improved exposure in multiple species following oral administration. benzamide 16-25 peroxisome proliferator activated receptor delta Homo sapiens 165-174 28756263-6 2017 Among them, compounds 7i, w, y with Cl, CN or NO2 groups at the 4-position of the benzamide scaffold showed excellent affinity for S1R (Ki = 1.2-3.6 nM), selectivity for S2R (Ki up to 1400 nM) and high selectivity index (IC50(SY5Y)/Ki(S1R) ratio from 28 000 to 83 000). benzamide 82-91 transmembrane BAX inhibitor motif containing 4 Homo sapiens 235-238 28415009-6 2017 Further modification of benzamide 3, 11a and 19 afforded new thienyl and phenyl compounds (50a, 50b, 63a, 63b and 63c) with dramatic HDAC1 and HDAC2 dual selectivity, and the fluorine containing compound 56, with moderate HDAC3 selectivity. benzamide 24-33 histone deacetylase 1 Homo sapiens 133-138 28415009-6 2017 Further modification of benzamide 3, 11a and 19 afforded new thienyl and phenyl compounds (50a, 50b, 63a, 63b and 63c) with dramatic HDAC1 and HDAC2 dual selectivity, and the fluorine containing compound 56, with moderate HDAC3 selectivity. benzamide 24-33 histone deacetylase 2 Homo sapiens 143-148 27250763-3 2016 4SC-202, a novel oral benzamide type HDAC inhibitor (HDACi) specific for class I HDACs HDAC1, HDAC2 and HDAC3 and the histone demethylase LSD1, shows substantial anti-tumor activity in a broad range of cancer cell lines and xenograft tumor models. benzamide 22-31 histone deacetylase 1 Homo sapiens 87-92 28174211-4 2017 For example, the benzamide class I HDAC-selective inhibitor, MGCD0103 [N-(2-aminophenyl)-4-[[(4-pyridin-3-ylpyrimidin-2-yl)amino]methyl] benzamide], was shown to block cardiac fibrosis, a process involving excess extracellular matrix deposition, which often results in heart dysfunction. benzamide 17-26 histone deacetylase 9 Homo sapiens 35-39 28501514-0 2017 Stabilizing HDAC11 with SAHA to assay slow-binding benzamide inhibitors. benzamide 51-60 histone deacetylase 11 Homo sapiens 12-18 28175303-0 2016 Friedreich ataxia-induced pluripotent stem cell-derived neurons show a cellular phenotype that is corrected by a benzamide HDAC inhibitor. benzamide 113-122 frataxin Homo sapiens 0-17 27297568-0 2016 Benzamide capped peptidomimetics as non-ATP competitive inhibitors of CDK2 using the REPLACE strategy. benzamide 0-9 cyclin dependent kinase 2 Homo sapiens 70-74 27548656-3 2016 Benzamide-substituted 2-pyridones are still by far the most popular selective EZH2 inhibitor class but alternative classes are now being reported. benzamide 0-9 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 78-82 28175303-4 2016 Treatment with the benzamide HDAC inhibitor 109 significantly upregulated FXN expression and increased Fe-S and lipoic acid-containing protein levels, downregulated SOD2 levels, normalized LIP and ROS levels, and almost fully protected FRDA neurons from oxidative stress-mediated cell death. benzamide 19-28 frataxin Homo sapiens 74-77 28175303-4 2016 Treatment with the benzamide HDAC inhibitor 109 significantly upregulated FXN expression and increased Fe-S and lipoic acid-containing protein levels, downregulated SOD2 levels, normalized LIP and ROS levels, and almost fully protected FRDA neurons from oxidative stress-mediated cell death. benzamide 19-28 superoxide dismutase 2 Homo sapiens 165-169 28175303-4 2016 Treatment with the benzamide HDAC inhibitor 109 significantly upregulated FXN expression and increased Fe-S and lipoic acid-containing protein levels, downregulated SOD2 levels, normalized LIP and ROS levels, and almost fully protected FRDA neurons from oxidative stress-mediated cell death. benzamide 19-28 frataxin Homo sapiens 236-240 27672541-3 2016 Chidamide (CS055) is a novel and orally active benzamide class of histone deacetylase (HDAC) inhibitor that selectively inhibits activity of HDAC1, 2, 3 and 10, the enzymes that are involved and play an important role in tumor initiation and development in both tumor cells and their surrounding micro-environment. benzamide 47-56 histone deacetylase 1 Homo sapiens 141-159 27208123-5 2016 The CDHB hydrolase (CbaA) was purified from strain DL-8, which can also hydrolyze 2-benzoxazolinone (BOA), 5-chloro-2-BOA, and benzamide. benzamide 127-136 cadherin 12 Homo sapiens 4-8 26590100-1 2016 The paper will describe the synthesis and SAR studies that led to the discovery of benzamide (reverse amide) as potent and selective human beta3-adrenergic receptor agonist. benzamide 83-92 adrenoceptor beta 3 Homo sapiens 139-164 26982372-3 2016 Linking benzamide substrates with a rotatable C-N bond, we constructed a novel semirigid pyramid-like scaffold that could support its two-turn alpha-helix mimicry without aromatic stacking interactions and could adopt the different dihedral angles of the key residues of p53 and BH3-only peptides. benzamide 8-17 tumor protein p53 Homo sapiens 271-274 27508038-2 2016 Chidamide, a novel HDAC inhibitor of the benzamide class, is currently under clinical trials. benzamide 41-50 histone deacetylase 9 Homo sapiens 19-23 27038494-0 2016 Selective non-zinc binding MMP-2 inhibitors: Novel benzamide Ilomastat analogs with anti-tumor metastasis. benzamide 51-60 matrix metallopeptidase 2 Homo sapiens 27-32 26731168-0 2016 Benzamide derivatives and their constrained analogs as histamine H3 receptor antagonists. benzamide 0-9 histamine receptor H3 Homo sapiens 55-76 26536614-10 2016 The benzamide compound, NBBA, exhibited a potent anti-IL-6 activity with inhibition of 35.6 +- 0.5%, significantly different from in the LPS-induced HGFs (p < 0.001). benzamide 4-13 interleukin 6 Homo sapiens 54-58 26613635-3 2015 The hybrids retained antiestrogenic and HDACi activity and, in the case of benzamide hybrids, were selective for Class I HDAC3 over Class II HDAC6. benzamide 75-84 histone deacetylase 6 Homo sapiens 141-146 26337021-0 2015 Discovery and SAR study of 3-(tert-butyl)-4-hydroxyphenyl benzoate and benzamide derivatives as novel farnesoid X receptor (FXR) antagonists. benzamide 71-80 nuclear receptor subfamily 1 group H member 4 Homo sapiens 102-122 26337021-0 2015 Discovery and SAR study of 3-(tert-butyl)-4-hydroxyphenyl benzoate and benzamide derivatives as novel farnesoid X receptor (FXR) antagonists. benzamide 71-80 nuclear receptor subfamily 1 group H member 4 Homo sapiens 124-127 26337021-3 2015 The results turn out that replacing the 2,4-dichlorophenyl with 2,6-dichloro-4-amidophenyl shows great improvement in potency, replacing the benzoate with benzamide shows improvement in stability and slight declining of potency and 3-(tert-butyl)-4-hydroxyphenyl unit is essential in obtaining the FXR antagonistic activity. benzamide 155-164 nuclear receptor subfamily 1 group H member 4 Homo sapiens 298-301 25981685-3 2015 Judicious selection of the substituents on the pyridine ring and benzamide groups led to 6b; which was highly potent, OX2R selective, and exhibited excellent development properties. benzamide 65-74 hypocretin receptor 2 Homo sapiens 118-122 25768700-2 2015 The evaluation of the regioisomers 11a-j highlighted a net increase of the anti-LSD1 potency by shifting the benzamide moiety from ortho to meta and mainly to para position of tranylcypromine phenyl ring, independently from their trans or cis stereochemistry. benzamide 109-118 lysine (K)-specific demethylase 1A Mus musculus 80-84