Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck II

被引：51

作者：

Burchat, AF

Calderwood, DJ

Hirst, GC

Holman, NJ

Johnston, DN

Munschauer, R

Rafferty, P

Tometzki, GB

机构：

[1] BASF Biores Corp, Worcester, MA 01605 USA

[2] BASF Pharma, Nottingham NG1 1GF, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 19期

关键词：

D O I：

10.1016/S0960-894X(00)00442-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Pyrrolo[2,3-d]pyrimidines containing a 5-(4-phenoxyphenyl) substituent are novel, potent and selective inhibitors of lck in vitro. Exploration of C-6 position of the pyrrolo[2,3-d]pyrimidine and the terminal phenyl group structure-activity relationship (SAR) is detailed. Compound 1 is orally active in animal models. (C) 2000 Elsevier Science Ltd. All rights reserved.

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页码：2171 / 2174

页数：4

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