Synthesis and biological evaluation of 2-amino-5-aryl-3-benzylthiopyridine scaffold based potent c-Met inhibitors

D Zhang, X Zhang, J Ai, Y Zhai, Z Liang, Y Wang…

Index: Zhang, Dengyou; Zhang, Xiaowei; Ai, Jing; Zhai, Yun; Liang, Zhongjie; Wang, Ying; Chen, Yi; Li, Chunpu; Zhao, Fei; Jiang, Hualiang; Geng, Meiyu; Luo, Cheng; Liu, Hong Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 21 p. 6804 - 6820

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Citation Number: 6

Abstract

Abstract A series of 2-amino-N-benzylpyridine-3-carboxnamides, 2-amino-N-benzylpyridine- 3-sulfonamides and 2-amino-3-benzylthiopyridines against c-Met were designed by means of bioisosteric replacement and docking analysis. Optimization of the 2-amino-3- benzylthiopyridine scaffold led to the identification of compound (R)-10b displaying c-Met inhibition with an IC 50 up to 7.7 nM. In the cytotoxic evaluation, compound (R)-10b ...