The discovery of N-(1,3-thiazol-2-yl)pyridin-2-amines as potent inhibitors of KDR kinase

被引：34

作者：

Bilodeau, MT

Rodman, LD

McGaughey, GB

Coll, KE

Koester, TJ

Hoffman, W

Hungate, LW

Kendall, RL

McFall, RC

Rickert, KW

Rutledge, RZ

Thomas, KA

机构：

[1] Merck Res Labs, Dept Med Chem, West Point, PA 19486 USA

[2] Merck Res Labs, Dept Mol Syst, West Point, PA 19486 USA

[3] Merck Res Labs, Dept Canc Res, West Point, PA 19486 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 11期

关键词：

KDR kinase; VEGF;

D O I：

10.1016/j.bmcl.2004.03.052

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

An azo-dye lead was modified to a novel N-(1,3-thiazol-2-yl)pyridin-2-amine series of KDR kinase inhibitors through the use of rapid analog libraries. This new class has been found to be potent, selective, and of low molecular weight. Molecular modeling has postulated an interesting conformational preference and binding mode for these compounds in the active site of the enzyme. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：2941 / 2945

页数：5

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