Synthesis of thiophene-2-carboxamidines containing 2-amino-thiazoles and their biological evaluation as urokinase inhibitors

被引：113

作者：

Wilson, KJ ^{[1
]}

Illig, CR ^{[1
]}

Subasinghe, N ^{[1
]}

Hoffman, JB ^{[1
]}

Rudolph, MJ ^{[1
]}

Soll, R ^{[1
]}

Molloy, CJ ^{[1
]}

Bone, R ^{[1
]}

Green, D ^{[1
]}

Randall, T ^{[1
]}

Zhang, M ^{[1
]}

Lewandowski, FA ^{[1
]}

Zhou, Z ^{[1
]}

Sharp, C ^{[1
]}

Maguire, D ^{[1
]}

Grasberger, B ^{[1
]}

DesJarlais, RL ^{[1
]}

Spurlino, J ^{[1
]}

机构：

[1] 3 Dimens Pharmaceut Inc, Exton, PA 19341 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 07期

关键词：

D O I：

10.1016/S0960-894X(01)00102-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The serine protease urokinase (uPa) has been implicated in the progression of both breast and prostate cancer. Utilizing structure based design, the synthesis of a series of substituted 4-[2-amino- 1,3-thiazolyl]-thiophene-2-carboxamidine is described. Further optimization of this series by substitution of the terminal amine yielded urokinase inhibitors with excellent activities. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：915 / 918

页数：4

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