… inhibition of 3, 5-disubstituted and 3, 5, 7-trisubstituted quinolines: identification of 3-(4-acetylpiperazin-1-yl)-5-(3-nitrobenzylamino)-7-(trifluoromethyl) quinoline as a …

Y Wang, J Ai, Y Wang, Y Chen, L Wang…

Index: Wang, Yuanxiang; Ai, Jing; Wang, Ying; Chen, Yi; Wang, Lu; Liu, Gang; Geng, Meiyu; Zhang, Ao Journal of Medicinal Chemistry, 2011 , vol. 54, # 7 p. 2127 - 2142

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Citation Number: 55

Abstract

By use of an improved synthetic strategy, a series of 3, 5-disubstituted and 3, 5, 7- trisubstituted quinolines were readily prepared. 3, 5, 7-Trisubstituted quinolines 21a− c, 21l, and 27a− c were identified as the most potent c-Met inhibitors with IC50 of less than 1.0 nM. Compound 21b showed the most promising overall PK profile and has high potency and extraordinary selectivity to c-Met against c-Met family member Ron and 12 other tyrosine ...