PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 30537230-2 2019 Here, we have demonstrated the ability of tilorone to activate NK cells and specific subpopulations of cytotoxic CD4+ and CD8+ T lymphocytes that recognize immune-evasive tumor cells and kill them via the FasL-Fas interaction. Tilorone 42-50 Fas ligand Homo sapiens 205-209 31094457-5 2019 RESULTS: A decrease in the frequency of ARVI in patients with CHF treated with Amixin was found, which was accompanied by a decrease in the severity of subclinical inflammation by reducing the production of proinflammatory (IL-1beta) and increasing the production of anti-inflammatory (IL-10) cytokines, reducing neurohumoral activation (reducing levels of aldosterone and Nt-proBNP), increasing the level of alpha- and gamma-interferon. Tilorone 79-85 interleukin 1 beta Homo sapiens 224-232 31094457-5 2019 RESULTS: A decrease in the frequency of ARVI in patients with CHF treated with Amixin was found, which was accompanied by a decrease in the severity of subclinical inflammation by reducing the production of proinflammatory (IL-1beta) and increasing the production of anti-inflammatory (IL-10) cytokines, reducing neurohumoral activation (reducing levels of aldosterone and Nt-proBNP), increasing the level of alpha- and gamma-interferon. Tilorone 79-85 interleukin 10 Homo sapiens 286-291 24841903-0 2014 Small-molecule screening of PC3 prostate cancer cells identifies tilorone dihydrochloride to selectively inhibit cell growth based on cyclin-dependent kinase 5 expression. Tilorone 65-89 chromobox 8 Homo sapiens 28-31 26633340-0 2015 An Effective Synthesis Method for Tilorone Dihydrochloride with Obvious IFN-alpha Inducing Activity. Tilorone 34-58 interferon alpha Mus musculus 72-81 26633340-5 2015 Furthermore, the synthesized tilorone dihydrochloride exhibited an obvious effect on induction of interferon-alpha (IFN-alpha) in mice within 12 h, and the peak level was observed until 24 h. This fruitful work has resulted in tilorone dihydrochloride becoming available in large-scale and wide application in clinics, which has a good pharmaceutical development prospects. Tilorone 29-53 interferon alpha Mus musculus 98-114 26633340-5 2015 Furthermore, the synthesized tilorone dihydrochloride exhibited an obvious effect on induction of interferon-alpha (IFN-alpha) in mice within 12 h, and the peak level was observed until 24 h. This fruitful work has resulted in tilorone dihydrochloride becoming available in large-scale and wide application in clinics, which has a good pharmaceutical development prospects. Tilorone 29-53 interferon alpha Mus musculus 116-125 26633340-5 2015 Furthermore, the synthesized tilorone dihydrochloride exhibited an obvious effect on induction of interferon-alpha (IFN-alpha) in mice within 12 h, and the peak level was observed until 24 h. This fruitful work has resulted in tilorone dihydrochloride becoming available in large-scale and wide application in clinics, which has a good pharmaceutical development prospects. Tilorone 227-251 interferon alpha Mus musculus 98-114 26633340-5 2015 Furthermore, the synthesized tilorone dihydrochloride exhibited an obvious effect on induction of interferon-alpha (IFN-alpha) in mice within 12 h, and the peak level was observed until 24 h. This fruitful work has resulted in tilorone dihydrochloride becoming available in large-scale and wide application in clinics, which has a good pharmaceutical development prospects. Tilorone 227-251 interferon alpha Mus musculus 116-125 24841903-0 2014 Small-molecule screening of PC3 prostate cancer cells identifies tilorone dihydrochloride to selectively inhibit cell growth based on cyclin-dependent kinase 5 expression. Tilorone 65-89 cyclin dependent kinase 5 Homo sapiens 134-159 24841903-6 2014 Screening of 3,360 compounds identified rutilantin, ethacridine lactate and cetalkonium chloride as compounds that selectively target PC3 control cells and a tilorone analog as a selective inhibitor of PC3 CDK5dn cells. Tilorone 158-166 chromobox 8 Homo sapiens 202-205 24841903-6 2014 Screening of 3,360 compounds identified rutilantin, ethacridine lactate and cetalkonium chloride as compounds that selectively target PC3 control cells and a tilorone analog as a selective inhibitor of PC3 CDK5dn cells. Tilorone 158-166 cyclin dependent kinase 5 Homo sapiens 206-210 24841903-8 2014 Validation experiments confirmed that tilorone treatment resulted in decreased PC3 cell growth and invasion; PC3 cells with inactive CDK5 were inhibited more effectively. Tilorone 38-46 chromobox 8 Homo sapiens 79-82 24841903-9 2014 Future studies are needed to unravel the mechanism of action of tilorone in CDK5 deficient prostate cancer cells and to test combination therapies with tilorone and a CDK5 inhibitor for its potential use in clinical practice. Tilorone 64-72 cyclin dependent kinase 5 Homo sapiens 76-80 22281189-0 2012 SAR of alpha7 nicotinic receptor agonists derived from tilorone: exploration of a novel nicotinic pharmacophore. Tilorone 55-63 sarcosine dehydrogenase Homo sapiens 0-3 23258233-0 2013 Bone morphogenetic protein-inducer tilorone identified by high-throughput screening is antifibrotic in vivo. Tilorone 35-43 bone morphogenetic protein 1 Homo sapiens 0-26 23258233-6 2013 The most promising drug candidate, tilorone, induced BMP signaling in the reporter cells and increased the expression of BMP-7 and a BMP target gene, Id3, in lung epithelial A549 cells. Tilorone 35-43 bone morphogenetic protein 1 Homo sapiens 53-56 23258233-6 2013 The most promising drug candidate, tilorone, induced BMP signaling in the reporter cells and increased the expression of BMP-7 and a BMP target gene, Id3, in lung epithelial A549 cells. Tilorone 35-43 bone morphogenetic protein 7 Mus musculus 121-126 23258233-6 2013 The most promising drug candidate, tilorone, induced BMP signaling in the reporter cells and increased the expression of BMP-7 and a BMP target gene, Id3, in lung epithelial A549 cells. Tilorone 35-43 bone morphogenetic protein 1 Homo sapiens 121-124 23258233-6 2013 The most promising drug candidate, tilorone, induced BMP signaling in the reporter cells and increased the expression of BMP-7 and a BMP target gene, Id3, in lung epithelial A549 cells. Tilorone 35-43 inhibitor of DNA binding 3 Mus musculus 150-153 23258233-7 2013 In a mouse model of pulmonary fibrosis, tilorone decreased lung hydroxyproline content and the expression of collagen genes Col1A1 and Col3A1. Tilorone 40-48 collagen, type I, alpha 1 Mus musculus 124-130 23258233-7 2013 In a mouse model of pulmonary fibrosis, tilorone decreased lung hydroxyproline content and the expression of collagen genes Col1A1 and Col3A1. Tilorone 40-48 collagen, type III, alpha 1 Mus musculus 135-141 18157163-5 2008 KEY RESULTS: Tilorone bound alpha7 nAChR (IC(50) 110 nM) with high selectivity relative to alpha4beta2 (IC(50) 70 000 nM), activated human alpha7 nAChR with an EC(50) value of 2.5 microM and maximal response of 67% relative to acetylcholine, and showed little agonist effect at human alpha3beta4 or alpha4beta2 nAChRs. Tilorone 13-21 cholinergic receptor nicotinic beta 1 subunit Rattus norvegicus 35-40 18157163-5 2008 KEY RESULTS: Tilorone bound alpha7 nAChR (IC(50) 110 nM) with high selectivity relative to alpha4beta2 (IC(50) 70 000 nM), activated human alpha7 nAChR with an EC(50) value of 2.5 microM and maximal response of 67% relative to acetylcholine, and showed little agonist effect at human alpha3beta4 or alpha4beta2 nAChRs. Tilorone 13-21 cholinergic receptor nicotinic beta 1 subunit Rattus norvegicus 146-151 18157163-9 2008 CONCLUSIONS AND IMPLICATIONS: Tilorone, known as an interferon inducer, is a selective alpha7 nAChR agonist, suggesting utility of the fluorenone pharmacophore for the development of alpha7 nAChR selective agonists. Tilorone 30-38 cholinergic receptor nicotinic beta 1 subunit Rattus norvegicus 94-99 18157163-9 2008 CONCLUSIONS AND IMPLICATIONS: Tilorone, known as an interferon inducer, is a selective alpha7 nAChR agonist, suggesting utility of the fluorenone pharmacophore for the development of alpha7 nAChR selective agonists. Tilorone 30-38 cholinergic receptor nicotinic beta 1 subunit Rattus norvegicus 190-195 12414762-5 2002 The results demonstrate that tilorone treatment elicits, by a direct effect, the production of proinflammatory cytokines (interleukin-6 [IL-6], tumor necrosis factor alpha [TNF-alpha], and IL-12) by splenic macrophages. Tilorone 29-37 interleukin 6 Mus musculus 122-135 18439305-6 2008 When an oral IFN-alpha inducer tilorone analog, R11567DA, was administered to SPF mice, IFN-alpha was induced rapidly in the LI at 4 h, whereas no IFN-alpha protein was detected in the small intestine (SI) or blood. Tilorone 31-39 interferon alpha Mus musculus 13-22 18439305-6 2008 When an oral IFN-alpha inducer tilorone analog, R11567DA, was administered to SPF mice, IFN-alpha was induced rapidly in the LI at 4 h, whereas no IFN-alpha protein was detected in the small intestine (SI) or blood. Tilorone 31-39 interferon alpha Mus musculus 88-97 18439305-6 2008 When an oral IFN-alpha inducer tilorone analog, R11567DA, was administered to SPF mice, IFN-alpha was induced rapidly in the LI at 4 h, whereas no IFN-alpha protein was detected in the small intestine (SI) or blood. Tilorone 31-39 interferon alpha Mus musculus 88-97 18028287-5 2008 A comparison of responses in naive mouse NK cells and NK cells pre-activated with the type I interferon-inducer tilorone demonstrated a dramatic influence of pre-activation, allowing potent degranulation and IFN-gamma responses to NKG2D mediated stimulation that were not observed with naive NK cells. Tilorone 112-120 interferon gamma Mus musculus 208-217 18028287-5 2008 A comparison of responses in naive mouse NK cells and NK cells pre-activated with the type I interferon-inducer tilorone demonstrated a dramatic influence of pre-activation, allowing potent degranulation and IFN-gamma responses to NKG2D mediated stimulation that were not observed with naive NK cells. Tilorone 112-120 killer cell lectin-like receptor subfamily K, member 1 Mus musculus 231-236 15848749-2 2005 In pursuing research on the antiviral, interferon (IFN)-inducing tilorone congeners, a new series of fluoren-carboxyhydroxyesters has been prepared and biologically explored. Tilorone 65-73 interferon alpha 1 Homo sapiens 51-54 12414762-5 2002 The results demonstrate that tilorone treatment elicits, by a direct effect, the production of proinflammatory cytokines (interleukin-6 [IL-6], tumor necrosis factor alpha [TNF-alpha], and IL-12) by splenic macrophages. Tilorone 29-37 interleukin 6 Mus musculus 137-141 12414762-5 2002 The results demonstrate that tilorone treatment elicits, by a direct effect, the production of proinflammatory cytokines (interleukin-6 [IL-6], tumor necrosis factor alpha [TNF-alpha], and IL-12) by splenic macrophages. Tilorone 29-37 tumor necrosis factor Mus musculus 144-171 12414762-5 2002 The results demonstrate that tilorone treatment elicits, by a direct effect, the production of proinflammatory cytokines (interleukin-6 [IL-6], tumor necrosis factor alpha [TNF-alpha], and IL-12) by splenic macrophages. Tilorone 29-37 tumor necrosis factor Mus musculus 173-182 1590774-5 1992 RNA blotting analysis demonstrates that interferon-alpha (IFN-alpha) and its inducers, i.e. poly(I).poly(C), bacterial lipopolysaccharide (LPS) and tilorone (2,7-bis-[2-(diethylamino)ethoxy]fluoren-9-one), increase the expression of XD mRNA in liver. Tilorone 148-156 interferon alpha Mus musculus 40-56 8287618-5 1994 The effect was not due to direct toxicity of the tilorone analog on tumor cells, but instead was dependent on NK cells; this was suggested by the finding that treatment of mice with anti-asialo GM1 abrogated the effect of the tilorone analog (RMI 10,874DA compound). Tilorone 49-57 coenzyme Q10A Mus musculus 194-197 8287618-5 1994 The effect was not due to direct toxicity of the tilorone analog on tumor cells, but instead was dependent on NK cells; this was suggested by the finding that treatment of mice with anti-asialo GM1 abrogated the effect of the tilorone analog (RMI 10,874DA compound). Tilorone 226-234 coenzyme Q10A Mus musculus 194-197 1590774-5 1992 RNA blotting analysis demonstrates that interferon-alpha (IFN-alpha) and its inducers, i.e. poly(I).poly(C), bacterial lipopolysaccharide (LPS) and tilorone (2,7-bis-[2-(diethylamino)ethoxy]fluoren-9-one), increase the expression of XD mRNA in liver. Tilorone 148-156 interferon alpha Mus musculus 58-67 2621325-0 1989 Potent inhibition of interleukin 1 beta-mediated human melanoma (A375.6) lysis by corticosteroids, staurosporine, and tilorone. Tilorone 118-126 interleukin 1 beta Homo sapiens 21-39 1567485-0 1992 Immunomodulation and drug acetylation: influence of the immunomodulator tilorone on hepatic, renal and blood N-acetyltransferase activity and on hepatic cytosolic acetyl coenzyme A content. Tilorone 72-80 N-acetyltransferase 1 Rattus norvegicus 109-128 1724584-2 1991 A comparative evaluation of L-1 (acridanon) and amixin (fluorenon) showed L-1 to have more marked interferon-inducing properties. Tilorone 48-54 L1 cell adhesion molecule Homo sapiens 74-77 1724584-4 1991 L-1 induced IF synthesis most actively after subcutaneous inoculation, amixin after oral administration. Tilorone 71-77 L1 cell adhesion molecule Homo sapiens 0-3 33778258-11 2021 We used microscale thermophoresis to test the binding of these molecules to the spike protein, and tilorone and pyronaridine bind to the spike receptor binding domain protein with K d values of 339 and 647 nM, respectively. Tilorone 99-107 surface glycoprotein Severe acute respiratory syndrome coronavirus 2 137-142 34705177-0 2021 Effect of Tilorone on the Dynamics of Viral Load and the Levels of Interferons and Interleukin-1beta in the Lung Tissue and Blood Serum of Mice with Experimental Influenza. Tilorone 10-18 interleukin 1 beta Mus musculus 83-100 34705177-1 2021 We studied the effect of tilorone on the dynamics of IFNalpha, IFNgamma, and IL-1beta levels in the lung tissue and blood serum in relation to viral load in the lungs of BALB/c mice with pneumonia caused by influenza virus A/Aichi/2/68 (H3N2). Tilorone 25-33 interferon alpha Mus musculus 53-61 34705177-1 2021 We studied the effect of tilorone on the dynamics of IFNalpha, IFNgamma, and IL-1beta levels in the lung tissue and blood serum in relation to viral load in the lungs of BALB/c mice with pneumonia caused by influenza virus A/Aichi/2/68 (H3N2). Tilorone 25-33 interferon gamma Mus musculus 63-71 34705177-1 2021 We studied the effect of tilorone on the dynamics of IFNalpha, IFNgamma, and IL-1beta levels in the lung tissue and blood serum in relation to viral load in the lungs of BALB/c mice with pneumonia caused by influenza virus A/Aichi/2/68 (H3N2). Tilorone 25-33 interleukin 1 alpha Mus musculus 77-85 3795024-1 1986 A wide variety of immunomodulators, including the synthetic interferon inducer tilorone (2,7-bis[2-(diethylamino)ethoxy]fluoren-9-one), have been shown to inhibit cytochrome P-450-dependent drug metabolism in vitro. Tilorone 79-87 cytochrome P450, family 2, subfamily g, polypeptide 1 Rattus norvegicus 163-179 3795024-1 1986 A wide variety of immunomodulators, including the synthetic interferon inducer tilorone (2,7-bis[2-(diethylamino)ethoxy]fluoren-9-one), have been shown to inhibit cytochrome P-450-dependent drug metabolism in vitro. Tilorone 89-133 cytochrome P450, family 2, subfamily g, polypeptide 1 Rattus norvegicus 163-179 2433236-9 1986 However, when given intranasally 7 days before an oral dose of tilorone, increased levels of IFN in lung suspensions are observed. Tilorone 63-71 interferon alpha 1 Homo sapiens 93-96 7215004-3 1981 Under defined experimental conditions tilorone hydrochloride also prevented pulmonary metastases from a subcutaneous tumour graft of epithelioma SP1 and mammary carcinoma SP22, as measured by an increased survival or treated rats. Tilorone 38-60 Parkinsonism associated deglycase Rattus norvegicus 171-175 6712731-7 1984 Thus, in maternal livers tilorone depressed cytochrome P-450 and AP N-demethylase activity in non-induced and PB-, MC- and PCN-induced rats and BP hydroxylase activity in the induced animals; BP hydroxylase activity was not depressed in non-induced maternal livers. Tilorone 25-33 cytochrome P450, family 2, subfamily g, polypeptide 1 Rattus norvegicus 44-60 6712731-10 1984 Fetal hepatic cytochrome P-450 and monooxygenase activities were increased by tilorone in PB- and PCN-induced rats but not in non-induced or MC-induced animals. Tilorone 78-86 cytochrome P450, family 2, subfamily g, polypeptide 1 Rattus norvegicus 14-30 6712732-8 1984 By day 7 postpartum, the cytochrome P-450 content and all three monooxygenase activities were depressed in rats that had received tilorone on days 1 and 2 postpartum. Tilorone 130-138 cytochrome P450, family 2, subfamily g, polypeptide 1 Rattus norvegicus 25-41 843913-8 1977 In passive EAE, the most significant increase occurred only in the lower spinal cord for cathepsins A and C, and fourthly, in monocytic EAE induced by tilorone, there was an exceptionally large, 3-fold increase in cathepsin C in lower cord as compared to a 1.5-2 fold increase for other cathepsins. Tilorone 151-159 cathepsin C Homo sapiens 214-225 6817439-2 1981 Inducers of alpha or beta (Type I) interferons, such as Tilorone-HCl, statalon, mengovirus and others, suppressed the cytochrome P-450 system of rats or mice after administration. Tilorone 56-68 cytochrome P450, family 21, subfamily a, polypeptide 1 Mus musculus 118-134 220421-0 1979 Reticuloendothelial cells as the site of production of MIF induced by tilorone hydrochloride. Tilorone 70-92 macrophage migration inhibitory factor Homo sapiens 55-58 17988-0 1977 Effect of tilorone hydrochloride on graft-versus-host (GvH) reaction in mice. Tilorone 10-32 graft versus host regulation Mus musculus 55-58 17988-1 1977 The effects of tilorone hydrochloride (TH), a powerful interferonogenic agent exhibiting also immune modulatory properties, on GvH reaction was studied, using the popliteal lymph node assay in mice. Tilorone 15-37 graft versus host regulation Mus musculus 127-130 17988-1 1977 The effects of tilorone hydrochloride (TH), a powerful interferonogenic agent exhibiting also immune modulatory properties, on GvH reaction was studied, using the popliteal lymph node assay in mice. Tilorone 39-41 graft versus host regulation Mus musculus 127-130 17988-4 1977 However, since normal parental lymphocytes are prepared for an enhanced GvH reactivity by addition of TH-treated macrophages, a stimulatory effect of the latter cells via macrophage-derived mediators, induced by TH, is suggested. Tilorone 102-104 graft versus host regulation Mus musculus 72-75 339871-2 1977 application of tilorone [2, 7-bis/2-diethylaminoethoxy/-fluoren-9-one dihydrochloride] to ABD2F1 mice demonstrated both interferon and migration inhibitory (MIF) activity. Tilorone 15-23 macrophage migration inhibitory factor (glycosylation-inhibiting factor) Mus musculus 157-160 339871-2 1977 application of tilorone [2, 7-bis/2-diethylaminoethoxy/-fluoren-9-one dihydrochloride] to ABD2F1 mice demonstrated both interferon and migration inhibitory (MIF) activity. Tilorone 25-85 macrophage migration inhibitory factor (glycosylation-inhibiting factor) Mus musculus 157-160 339871-4 1977 The physiochemical characteristics of tilorone-induced MIF (heat and pH lability, molecular size) are compared with those of MIF generated in in vitro lymphocyte cultures. Tilorone 38-46 macrophage migration inhibitory factor (glycosylation-inhibiting factor) Mus musculus 55-58 6226-0 1976 Depression of the hepatic cytochrome P-450 mono-oxygenase system by administered tilorone (2,7-bis(2-(diethylamino)ethoxy)fluoren-9-one dihydrochloride). Tilorone 81-89 cytochrome P450, family 2, subfamily j, polypeptide 3 Rattus norvegicus 26-57 6226-0 1976 Depression of the hepatic cytochrome P-450 mono-oxygenase system by administered tilorone (2,7-bis(2-(diethylamino)ethoxy)fluoren-9-one dihydrochloride). Tilorone 91-151 cytochrome P450, family 2, subfamily j, polypeptide 3 Rattus norvegicus 26-57 6226-3 1976 After a single oral dose of tilorone-HCl (50 mg/kg) a loss of 38% of the microsomal cytochrome P-450 and 25% of the ethylmorphine N-demethylase activity was observed within 24 hr; recovery was complete within 8 to 10 days. Tilorone 28-40 cytochrome P450, family 2, subfamily g, polypeptide 1 Rattus norvegicus 84-100 6226-5 1976 In vitro, tilorone-HCl showed no inhibitory effect on microsomal drug metabolism nod did it affect the cytochrome P-450 content of the microsomes. Tilorone 10-22 cytochrome P450, family 2, subfamily g, polypeptide 1 Rattus norvegicus 103-119 33400519-0 2021 The Antiviral Drug Tilorone Is a Potent and Selective Inhibitor of Acetylcholinesterase. Tilorone 19-27 acetylcholinesterase (Cartwright blood group) Homo sapiens 67-87 1200845-0 1975 Comparison of the ability of small molecular interferon inducers: tilorone and acridine drugs. Tilorone 66-74 interferon Gallus gallus 45-55 1200845-3 1975 Acranil, given parenterally, proved to be as strong as tilorone regarding interferon stimulation, in spite of the presence of only one side chain in the Acrainl molecule. Tilorone 55-63 interferon Gallus gallus 74-84 33400519-4 2021 High-throughput screens for the eel AChE inhibitor model identified several molecules including tilorone, an antiviral drug that is well-established outside of the United States, as a newly identified nanomolar AChE inhibitor. Tilorone 96-104 acetylcholinesterase (Cartwright blood group) Homo sapiens 36-40 33400519-4 2021 High-throughput screens for the eel AChE inhibitor model identified several molecules including tilorone, an antiviral drug that is well-established outside of the United States, as a newly identified nanomolar AChE inhibitor. Tilorone 96-104 acetylcholinesterase (Cartwright blood group) Homo sapiens 211-215 33400519-8 2021 This study suggests there may be a potential role for repurposing tilorone or its derivatives in conditions that benefit from AChE inhibition. Tilorone 66-74 acetylcholinesterase (Cartwright blood group) Homo sapiens 126-130