Discovery of a novel and potent series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases

被引：68

作者：

Claridge, Stephen ^{[1
]}

Raeppel, Franck ^{[1
]}

Granger, Marie-Claude ^{[1
]}

Bernstein, Naomy ^{[1
]}

Saavedra, Oscar ^{[1
]}

Zhan, Lijie ^{[1
]}

Llewellyn, David ^{[1
]}

Wahhab, Amal ^{[1
]}

Deziel, Robert ^{[1
]}

Rahil, Jubrail ^{[3
]}

Beaulieu, Normand ^{[2
]}

Nguyen, Hannah ^{[2
]}

Dupont, Isabelle ^{[2
]}

Barsalou, Annie ^{[2
]}

Beaulieu, Carole ^{[2
]}

Chute, Ian ^{[2
]}

Gravel, Serge ^{[2
]}

Robert, Marie-France ^{[2
]}

Lefebvre, Sylvain ^{[2
]}

Dubay, Marja ^{[2
]}

Pascal, Roussen ^{[4
]}

Gillespie, Jeff ^{[4
]}

Jin, Zhiyun ^{[4
]}

Wang, James ^{[4
]}

Besterman, Jeffrey M. ^{[2
]}

MacLeod, A. Robert ^{[2
]}

Vaisburg, Arkadii ^{[1
]}

机构：

[1] MethylGene Inc, Dept Med Chem, Montreal, PQ H4S 2A1, Canada

[2] MethylGene Inc, Dept Cell Biol & Pharmacol, Montreal, PQ H4S 2A1, Canada

[3] MethylGene Inc, Dept Lead Discovery, Montreal, PQ H4S 2A1, Canada

[4] MethylGene Inc, Dept PK Analyt Chem, Montreal, PQ H4S 2A1, Canada

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 09期

关键词：

c-Met; VEGFR2; kinase; thieno[3,2-b]pyridine; cancer;

D O I：

10.1016/j.bmcl.2008.04.009

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases is described. The compounds demonstrated potency with IC50 values in the low nanomolar range in vitro while the lead compound also showed in vivo activity against various human tumor xenograft models in mice. Further exploration of this class of compounds is underway. (c) 2008 Elsevier Ltd. All rights reserved.

引用

页码：2793 / 2798

页数：6

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