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

被引：44

作者：

Tang, Qidong ^{[1
,3
]}

Wang, Linxiao ^{[1
]}

Tu, Yayi ^{[1
]}

Zhu, Wufu ^{[1
]}

Luo, Rong ^{[2
]}

Tu, Qidong ^{[1
]}

Wang, Ping ^{[1
]}

Wu, Chunjiang ^{[1
]}

Gong, Ping ^{[3
]}

Zheng, Pengwu ^{[1
]}

机构：

[1] Jiangxi Sci & Technol Normal Univ, Sch Pharm, Nanchang 330013, Peoples R China

[2] Jiangxi Prov Inst Mat Med, Nanchang 330000, Peoples R China

[3] Shenyang Pharmaceut Univ, Sch Pharmaceut Engn, Key Lab Struct Based Drug Design & Discovery, Minist Educ, Shenyang 110016, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2016年 / 26卷 / 07期

关键词：

Synthesis; Pyrrolo[2,3-b]pyridine derivatives; 1,2,3-Triazole; c-Met; Antiproliferative activity; PROSTATE-CANCER; DESIGN; IDENTIFICATION; GROWTH;

D O I：

10.1016/j.bmcl.2016.02.059

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

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.

引用

页码：1680 / 1684

页数：5

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