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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
Authors:Lianbao Ye  Yuanxin Tian  Zhonghuang Li  Jiajie Zhang  Shuguang Wu
Affiliation:1. School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, P.?R. China, (phone: +86‐20‐62789415;2. fax: +86‐20‐61648548)
Abstract: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 4a – 4c 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 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.
Keywords:c‐Met Inhibitor  1H‐Pyrido[4,3‐b]indoles, 2,3,4,5‐tetrahydro‐  Suzuki coupling reaction  Inhibitors  Tyrosine‐kinase receptor
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