Synthesis and in vitro evaluation of a series of diketopiperazine inhibitors of plasminogen activator inhibitor-1

被引：57

作者：

Folkes, A ^{[1
]}

Roe, MB ^{[1
]}

Sohal, S ^{[1
]}

Golec, J ^{[1
]}

Faint, R ^{[1
]}

Brooks, T ^{[1
]}

Charlton, P ^{[1
]}

机构：

[1] Xenova Ltd, Slough SL1 4NL, Berks, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 19期

关键词：

D O I：

10.1016/S0960-894X(01)00508-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We have synthesized and evaluated a series of diketopiperazine-based inhibitors of PAI-1. These studies resulted in the identification of 34 which inhibited PAI-1 in vitro with an IC50 = 0.2 muM. The synthesis and SAR of these compounds are described. (C) 2001 Elsevier Science Ltd. All rights reserved.

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页码：2589 / 2592

页数：4

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