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Discovery of novel pyrrolo[2,3-b]pyridine derivatives bearing 1,2,3-triazole moiety as c-Met kinase inhibitors

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2016)

期刊

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷 26, 期 7, 页码 1680-1684

出版社

PERGAMON-ELSEVIER SCIENCE LTD

DOI: 10.1016/j.bmcl.2016.02.059

关键词

Synthesis; Pyrrolo[2,3-b]pyridine derivatives; 1,2,3-Triazole; c-Met; Antiproliferative activity

类别

Chemistry, Medicinal Chemistry, Organic

资金

Research Fund for the Doctoral Program of Jiangxi Science and Technology Normal University [3000990116]

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摘要

A series of novel pyrrolo[2,3-b]pyridine derivatives bearing 1,2,3-triazole moiety were designed, synthesized, and evaluated for their c-Met kinase inhibitory activities and antiproliferative activities against 4 cancer cell lines (HT-29, A549, MCF-7, and PC-3) in vitro. Most compounds showed moderate to excellent potency, with the most promising analog 34 showing a c-Met IC50 value of 1.68 nM. Structure-activity relationship studies indicated that electron-withdrawing groups (X = CF3, R-1 = F, R-2 = 4-F) were required to decrease the higher electron density on the 5-atom linker to a proper degree to improve the inhibitory activity. (C) 2016 Elsevier Ltd. All rights reserved.

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