Inhibition of estrone sulfatase (ES) by derivatives of 4-[(aminosulfonyl)oxy] benzoic acid

被引：20

作者：

Ahmed, S

James, K

Owen, CP

机构：

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

[2] Inst Canc Res, Surrey, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 17期

关键词：

D O I：

10.1016/S0960-894X(02)00383-9

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 straight chain alkyl esters of 4-[(aminosulfonyl)oxy] benzoic acid. The results of the study show that the synthesised compounds possess greater inhibitory activity when compared to COUMATE, although they were all found to possess lower inhibitory activity with respect to EMATE. Furthermore, the data suggest a strong correlation between logP and IC50 and therefore adds further support to our previous report where we suggested a link between inhibitory activity and hydrophobicity. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：2391 / 2394

页数：4

共 8 条

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