Pyrazolo[3,4-d]pyrimidines containing an extended 3-substituent as potent inhibitors of Lck -: a selectivity insight

被引：63

作者：

Burchat, AF ^{[1
]}

Calderwood, DJ ^{[1
]}

Friedman, MM ^{[1
]}

Hirst, GC ^{[1
]}

Li, BQ ^{[1
]}

Rafferty, P ^{[1
]}

Ritter, K ^{[1
]}

Skinner, BS ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 12期

关键词：

D O I：

10.1016/S0960-894X(02)00196-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of para-substituted 3-phenyl pyrazolopyrimidines was synthesized and evaluated as inhibitors of lck. The nature of the substitution affected enzyme selectivity and potency for lck, src, kdr, and tie-2. The para-phenoxyphenyl analogue 2 is an orally active lck inhibitor with a bioavailability of 69% and exhibits an extended duration of action in animal models of T cell inhibition. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：1687 / 1690

页数：4

共 14 条

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