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Design and Synthesis of Some Novel 2,3,4,5-Tetrahydro-1H-pyrido[4,3-b]indoles as Potential c-Met Inhibitors

Journal 2012 · IF 1.478 · 95(2): 320-326 · 发表于 2012 年 2 月 16 日
作者: Lianbao Ye,Yuanxin Tian,Zhonghuang Li,Jiajie Zhang,Shuguang Wu
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摘要

Since deregulation of the tyrosine-kinase receptor c-Met is implicated in several human cancers and is an attractive target for small-molecule-drug discovery, we report herein the synthesis of 2,3,4,5-tetrahydro-8-[1-(quinolin-6-ylmethyl)-1 H -1,2,3-triazolo[4,5- b ]pyrazin-6-yl]-1 H -pyrido[4,3- b ]indoles 4a – 4c and 2,3,4,5-tetrahydro-8-[3-(quinolin-6-ylmethyl)-1,2,4-triazolo[4,3- b ]pyridazin-6-yl]-1 H -pyrido[4,3-b]indoles 5a – 5c . These indole derivatives demonstrated inhibition of c-Met kinase activity. Concurrently, five key intermediates were synthesized. These compounds could be prepared in good yields.