Inhibition of estrone sulfatase (ES) by alkyl and cycloalkyl ester derivatives of 4-[(aminosulfonyl)oxyl benzoic acid

被引：26

作者：

Patel, CK ^{[1
]}

Owen, CP ^{[1
]}

Ahmed, S ^{[1
]}

机构：

[1] Kingston Univ, Sch Chem & Pharmaceut Sci, Dept Pharm, Kingston upon Thames KT1 2EE, Surrey, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 03期

关键词：

D O I：

10.1016/j.bmcl.2003.11.067

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In our search for potent inhibitors of the enzyme estrone sulfatase (ES), we have undertaken the synthesis and biochemical evaluation of a range of esters of 4-[(aminosulfonyl)oxy] benzoic acid. The results of the study show that the synthesised compounds possess potent inhibitory activity, indeed the cyclooctyl derivative was found to be more potent than 667-COUMATE, which is currently undergoing clinical trials. (C) 2003 Elsevier Ltd. All rights reserved.

引用

页码：605 / 609

页数：5

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