The discovery of potent cRaf1 kinase inhibitors

被引：193

作者：

Lackey, K ^{[1
]}

Cory, M ^{[1
]}

Davis, R ^{[1
]}

Frye, SV ^{[1
]}

Harris, PA ^{[1
]}

Hunter, RN ^{[1
]}

Jung, DK ^{[1
]}

McDonald, OB ^{[1
]}

McNutt, RW ^{[1
]}

Peel, MR ^{[1
]}

Rutkowske, RD ^{[1
]}

Veal, JM ^{[1
]}

Wood, ER ^{[1
]}

机构：

[1] Glaxo Wellcome Inc, Res Triangle Pk, NC 27709 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 03期

关键词：

D O I：

10.1016/S0960-894X(99)00668-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of benzylidene-1H-indol-2-one (oxindole) derivatives was synthesized and evaluated as cRaf-1 kinase inhibitors. The key features of the molecules were the donor/acceptor motif common to kinase inhibitors and a critical acidic phenol flanked by two substitutions. Diverse 5-position substitutions provided compounds with low nanomolar kinase enzyme inhibition and inhibited the intracellular MAPK pathway. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：223 / 226

页数：4

共 17 条

[1] RAF MEETS RAS - COMPLETING THE FRAMEWORK OF A SIGNAL-TRANSDUCTION PATHWAY [J].