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

Ahmed, Sabbir, James, Karen and Owen, Caroline P. (2002) Inhibition of estrone sulfatase (ES) by derivatives of 4-[(aminosulfonyl)oxy] benzoic acid. Bioorganic & Medicinal Chemistry Letters, 12(17), pp. 2391-2394. ISSN (print) 0960-894X

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Abstract

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 IC(50) and therefore adds further support to our previous report where we suggested a link between inhibitory activity and hydrophobicity.

Item Type: Article
Uncontrolled Keywords: aromatase inhibitors
Research Area: Chemistry
Faculty, School or Research Centre: Faculty of Science (until 2011) > School of Pharmacy and Chemistry
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Depositing User: Automatic Import Agent
Date Deposited: 10 Mar 2010 15:54
Last Modified: 19 Nov 2010 14:46
URI: http://eprints.kingston.ac.uk/id/eprint/7197

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