Design, synthesis and biological evaluation of novel imidazo [4, 5-c] pyridinecarboxamide derivatives as PARP-1 inhibitors

Q Zhu, X Wang, Z Chu, G He, G Dong, Y Xu

Index: Zhu, Qihua; Wang, Xuyan; Chu, Zhaoxing; He, Guangwei; Dong, Guangping; Xu, Yungen Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 7 p. 1993 - 1996

Full Text: HTML

Citation Number: 15

Abstract

A series of novel cyclic amine-substituted imidazo [4, 5-c] pyridinecarboxamide analogs were designed and synthesized. All the target compounds were evaluated for their PARP inhibition activity, and the result indicated that most of the compounds possessed inhibitory effect on PARP at the concentration of 1μM, among which compound 8d (IC50= 0.528 μM) was selected for evaluating the antitumor effect in vivo. The result showed the antitumor ...