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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

Ye Lianbao; Tian Yuanxin; Li Zhonghuang; Zhang Jiajie*; Wu Shuguang
SCI
南方医科大学

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)-1H-1,2,3-triazolo[4,5-b]pyrazin-6-yl]-1H-pyrido[4,3-b]indoles 4a4c and 2,3,4,5-tetrahydro-8-[3-(quinolin-6-ylmethyl)-1,2,4-triazolo[4,3-b]pyridazin-6-yl]-1H-pyrido[4,3-b]indoles 5a5c. These indole derivatives demonstrated inhibition of c-Met kinase activity. Concurrently, five key intermediates were synthesized. These compounds could be prepared in good yields.

关键词

c-Met Inhibitor 1H-Pyrido[4 3-b]indoles 2 3 4 5-tetrahydro- Suzuki coupling reaction Inhibitors Tyrosine-kinase receptor