Isoindolinone ureas: a novel class of KDR kinase inhibitors

被引：33

作者：

Curtin, ML

Frey, RR

Heyman, HR

Sarris, KA

Steinman, DH

Holmes, JH

Bousquet, PF

Cunha, GA

Moskey, MD

Ahmed, AA

Pease, LJ

Glaser, KB

Stewart, KD

Davidsen, SK

Michaelides, MR

机构：

[1] Abbott Labs, Abbott Pk, IL 60064 USA

[2] Abbott Biores Ctr, Worcester, MA 01605 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 17期

关键词：

KDR kinase; VEGF; isoindolinone; urea;

D O I：

10.1016/j.bmcl.2004.06.041

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of substituted isoindolinone ureas was prepared and evaluated for enzymatic and cellular inhibition of KDR kinase activity. Several of these analogs, such as 14c, are potent inhibitors of KDR both enzymatically (<50nM) and cellularly (less than or equal to100 nM). A 3D KDR/CDK2/MAP kinase overlay model with several structurally related tyrosine kinase inhibitors was used to predict the binding interactions of the isoindolinone ureas with the KDR active site. (C) 2004 Elsevier Ltd. All rights reserved.

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收藏

页码：4505 / 4509

页数：5

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