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

Patel, Chirag K., Owen, Caroline P. and Ahmed, Sabbir (2004) Inhibition of estrone sulfatase (ES) by alkyl and cycloalkyl ester derivatives of 4-[(aminosulfonyl)oxy] benzoic acid. Bioorganic & Medicinal Chemistry Letters, 14(3), pp. 605-609. 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 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.

Item Type: Article
Uncontrolled Keywords: physicochemical factor, biochemical evaluation
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: 06 Jan 2012 13:21
URI: http://eprints.kingston.ac.uk/id/eprint/1384

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