发现一系列新型且强效的基于噻吩并[3,2-b]吡啶的c-Met和VEGFR2酪氨酸激酶抑制剂。

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

作者信息

Claridge Stephen, Raeppel Franck, Granger Marie-Claude, Bernstein Naomy, Saavedra Oscar, Zhan Lijie, Llewellyn David, Wahhab Amal, Deziel Robert, Rahil Jubrail, Beaulieu Normand, Nguyen Hannah, Dupont Isabelle, Barsalou Annie, Beaulieu Carole, Chute Ian, Gravel Serge, Robert Marie-France, Lefebvre Sylvain, Dubay Marja, Pascal Roussen, Gillespie Jeff, Jin Zhiyun, Wang James, Besterman Jeffrey M, MacLeod A Robert, Vaisburg Arkadii

机构信息

Department of Medicinal Chemistry, MethylGene Inc., 7220 Frederick-Banting, Montréal, Que., Canada H4S 2A1.

出版信息

Bioorg Med Chem Lett. 2008 May 1;18(9):2793-8. doi: 10.1016/j.bmcl.2008.04.009. Epub 2008 Apr 9.

DOI:10.1016/j.bmcl.2008.04.009

PMID:18434145

Abstract

A series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases is described. The compounds demonstrated potency with IC(50) 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.

摘要

描述了一系列基于噻吩并[3,2 - b]吡啶的c - Met和VEGFR2酪氨酸激酶抑制剂。这些化合物在体外表现出效力，IC(50)值处于低纳摩尔范围，而先导化合物在小鼠体内对各种人类肿瘤异种移植模型也显示出活性。对这类化合物的进一步探索正在进行中。

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发现一系列新型且强效的基于噻吩并[3,2-b]吡啶的c-Met和VEGFR2酪氨酸激酶抑制剂。

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

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发现一系列新型且强效的基于噻吩并[3,2-b]吡啶的c-Met和VEGFR2酪氨酸激酶抑制剂。

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

作者信息

机构信息

出版信息