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

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

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被引用次数: 15

摘要

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 ...