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Bioorg Med Chem Lett. 2013 Apr 1;23(7):1993-6. doi: 10.1016/j.bmcl.2013.02.032. Epub 2013 Feb 16.

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

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Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 21009, China.


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 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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