Design, synthesis and in vitro evaluation of potent, novel, small molecule inhibitors of plasminogen activator inhibitor-1

被引：27

作者：

Folkes, A

Brown, SD

Canne, LE

Chan, J

Engelhardt, E

Epshteyn, S

Faint, R

Golec, J

Hanel, A

Kearney, P

Leahy, JW

Mac, M

Matthews, D

Prisbylla, MP

Sanderson, J

Simon, RJ

Tesfai, Z

Vicker, N

Wang, SM

Webb, RR

Charlton, P

机构：

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

[2] Metaxen, San Francisco, CA 94080 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 07期

关键词：

D O I：

10.1016/S0960-894X(02)00078-1

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 tetramic acid-based and hydroxvquinolinone-based inhibitors of plasminogen activator inhibitor-1 (PAI-1). These studies resulted in the identification of several compounds which showed excellent potency against PAI-1. The design, synthesis and SAR of these compounds are described. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：1063 / 1066

页数：4

共 18 条

[1]

AZNAR J, 1994, HAEMOSTASIS, V24, P243

[2] Absence of host plasminogen activator inhibitor 1 prevents cancer invasion and vascularization [J].