1-Phenyl-5-pyrazolyl ureas: Potent and selective p38 kinase inhibitors

被引：71

作者：

Dumas, J

Hatoum-Mokdad, H

Sibley, R

Riedl, B

Scott, WJ

Monahan, MK

Lowinger, TB

Brennan, C

Natero, R

Turner, T

Johnson, JS

Schoenleber, R

Bhargava, A

Wilhelm, SM

Housley, TJ

Ranges, GE

Shrikhande, A

机构：

[1] Bayer Res Ctr, Dept Chem Res, W Haven, CT 06516 USA

[2] Bayer Res Ctr, Dept Canc & Osteoporosis Res, W Haven, CT 06516 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 18期

关键词：

D O I：

10.1016/S0960-894X(00)00272-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Inhibitors of the MAP kinase p38 are potentially useful for the treatment of arthritis and osteoporosis. Several 2,3-dichlorophenyl ureas were identified as small-molecule inhibitors of p38 by a combinatorial chemistry effort. Optimization for cellular potency led to the discovery of a new class of potent and selective p38 kinase inhibitors, exemplified by the 1-phenyl-5-pyrazolyl urea 7 (IC50 = 13 nM). (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：2051 / 2054

页数：4

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