Title : Recent Progress of the research on the benzimidazole PARP-1 inhibitors.

Pub. Date : 2022 Mar 21

PMID : 35319364






6 Functional Relationships(s)
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1 Recent Progress of the research on the benzimidazole PARP-1 inhibitors. benzimidazole poly(ADP-ribose) polymerase 1 Homo sapiens
2 However, the commercial available benzimidazole PARP-1 inhibitors have some shortcomings such as serious toxicity in combination with chemotherapy drugs, in vivo cardiovascular side effects such as anemia. benzimidazole poly(ADP-ribose) polymerase 1 Homo sapiens
3 Therefore it"s crucial for scientists to explore more structure-activity relationships of the benzimidazole PARP-1 inhibitors and access safer and more effective PARP inhibitors. benzimidazole poly(ADP-ribose) polymerase 1 Homo sapiens
4 As the binding region of PARP-1 and the substrates is usually characterized as NI site and AD site, the modification of benzimidazoles mainly occurs on the benzimidazole skeleton (NI site), and the side chain of benzimidazole on 2-C position (AD site). benzimidazole poly(ADP-ribose) polymerase 1 Homo sapiens
5 As the binding region of PARP-1 and the substrates is usually characterized as NI site and AD site, the modification of benzimidazoles mainly occurs on the benzimidazole skeleton (NI site), and the side chain of benzimidazole on 2-C position (AD site). benzimidazole poly(ADP-ribose) polymerase 1 Homo sapiens
6 We hope that enlightened by the previous researches, more researches of AD site should be occurred and more effective benzimidazole PARP-1 inhibitors could be designed, synthesized, and applied to clinics. benzimidazole poly(ADP-ribose) polymerase 1 Homo sapiens