Hydrophobicity, a physicochemical factor in the inhibition of the enzyme estrone sulfatase (ES)

被引：21

作者：

Ahmed, S ^{[1
]}

James, K ^{[1
]}

Owen, CP ^{[1
]}

Patel, CK ^{[1
]}

Patel, M ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 18期

关键词：

D O I：

10.1016/S0960-894X(01)00482-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We report the initial structure-activity relationship study (SAR) (in particular log P) of a series of compounds based upon 4-sulfamated phenyl ketones as potent inhibitors of the enzyme estrone sulfatase (ES). The results of the study show that these compounds are irreversible inhibitors of ES and that they are more potent than COUMATE, but weaker than ENTATE. Analysis of the SAR data shows a strong correlation between IC50 and log P but also supports our previous study, which suggests a very strong relationship between pK(a) and IC50. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：2525 / 2528

页数：4

共 9 条

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