The design, synthesis, and in vitro biochemical evaluation of a series of esters of 4-[(aminosulfonyl)oxy]benzoate as novel and highly potent inhibitors of estrone sulfatase

Patel, Chirag K., Owen, Caroline P. and Ahmed, Sabbir (2003) The design, synthesis, and in vitro biochemical evaluation of a series of esters of 4-[(aminosulfonyl)oxy]benzoate as novel and highly potent inhibitors of estrone sulfatase. Biochemical and Biophysical Research Communications, 307(4), pp. 778-781. ISSN (print) 0006-291X

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Abstract

We report the initial results of our study into the use of a potential transition-state (TS) of the reaction catalysed by the enzyme estrone sulfatase (ES) in the design of a series of cyclic esters of 4-[(aminosulfonyl)oxy]benzoate as novel inhibitors of ES. The results of the study show that these compounds are some of the most potent inhibitors known todate, possessing greater inhibitory activity than the three standard compounds: 4-methylcoumarin-7-O-sulfamate (COUMATE); the tricyclic derivative of COUMATE, namely 667-COUMATE (which is in Phase I of clinical trials) and; the steroidal inhibitor estrone-3-O-sulfamate (EMATE).

Item Type: Article
Uncontrolled Keywords: steroid sulfatase, estrone-3-o-sulfamate, es
Research Area: Allied health professions and studies
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: 26 Jun 2007
Last Modified: 06 Jan 2012 13:25
URI: http://eprints.kingston.ac.uk/id/eprint/1532

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