Discovery and evaluation of 3-(5-thien-3-ylpyridin-3-yl)-1H-indoles as a novel class of KDR kinase inhibitors

被引：11

作者：

Fraley, ME ^{[1
]}

Arrington, KL

Hambaugh, SR

Hoffman, WF

Cunningham, AM

Young, MB

Hungate, RW

Tebben, AJ

Rutledge, RZ

Kendall, RL

Huckle, WR

McFall, RC

Coll, KE

Thomas, KA

机构：

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

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 18期

关键词：

D O I：

10.1016/S0960-894X(03)00627-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We have discovered 3-(5-thien-3-ylpyridin-3-yl)-1H-indoles as potent inhibitors of KDR kinase activity. This communication details the evolution of this novel class from a potent screening lead of vastly different structure with an emphasis on structural modifications that retained activity and provided improvements in key physical properties. The synthesis and in-depth evaluation of these inhibitors are described. (C) 2003 Elsevier Ltd. All rights reserved.

引用

页码：2973 / 2976

页数：4

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