Discovery of novel 2-aminopyridine-3-carboxamides as c-Met kinase inhibitors

…, Z Liang, C Li, X Peng, YC Ji, H Jiang, M Geng…

Index: Zhang, Dengyou; Ai, Jing; Liang, Zhongjie; Li, Chunpu; Peng, Xia; Ji, Yinchun; Jiang, Hualiang; Geng, Meiyu; Luo, Cheng; Liu, Hong Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 17 p. 5169 - 5180

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Citation Number: 13

Abstract

A series of 2-aminopyridine-3-carboxamide derivatives against c-Met were designed and synthesized by employing bioisosteric replacement of heterocyclic moieties with the amide bond. The structure–activity relationship (SAR) at various positions of the scaffold was explored. In this study, a promising compound (S)-24o with a c-Met IC50 of 0.022 μM was identified. The compound exhibited dose-dependent inhibition of the phosphorylation of c- ...