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

Ahmed, Sabbir, James, Karen, Owen, Caroline P., Patel, Chirag and Patel, Mijal (2001) Hydrophobicity, a physicochemical factor in the inhibition of the enzyme estrone sulfatase (ES). Bioorganic & Medicinal Chemistry Letters, 11(18), pp. 2525-2528. ISSN (print) 0960-894X

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Abstract

We report the initial structure-activity relationship study (SAR) (in particular logP) 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 EMATE. Analysis of the SAR data shows a strong correlation between IC(50) and logP but also supports our previous study, which suggests a very strong relationship between pK(a) and IC(50).

Item Type: Article
Uncontrolled Keywords: aromatase inhibitors, steroid sulfatase
Research Area: Chemistry
Faculty, School or Research Centre: Faculty of Science (until 2011) > School of Pharmacy and Chemistry
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Depositing User: David Salliss
Date Deposited: 19 Jun 2007
Last Modified: 14 Apr 2011 12:07
URI: http://eprints.kingston.ac.uk/id/eprint/1382

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