Design,synthesis and biological evaluation of novel imidazo[4,5-c]pyridinecarboxamide derivatives as PARP-1 inhibitors |
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| Authors: | Qihua Zhu Xuyan Wang Zhaoxing Chu Guangwei He Guangping Dong Yungen Xu |
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| Institution: | 1. Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 21009, China;2. Hefei YiGong Pharmaceutical Co. Ltd, Hefei 230088, China |
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| Abstract: | A series of novel cyclic amine-substituted imidazo4,5-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 1 μM, among which compound 8d (IC50 = 0.528 μM) was selected for evaluating the antitumor effect in vivo. The result showed the antitumor efficacy of the compound 8d and cisplatin combination group in a mouse A549 model is similar with that of the ABT-888 and cisplatin combination group. |
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