Design, synthesis and biochemical evaluation of AC ring mimics as novel inhibitors of the enzyme estrone sulfatase (ES)

Ahmed, Sabbir, James, Karen, Owen, Caroline P. and Patel, Chirag K. (2002) Design, synthesis and biochemical evaluation of AC ring mimics as novel inhibitors of the enzyme estrone sulfatase (ES). Bioorganic & Medicinal Chemistry Letters, 12(10), pp. 1343-1346. ISSN (print) 0960-894X

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Abstract

We report the initial results of our study into a series of simple 4'-O-sulfamoyl-4-biphenyl based compounds as novel inhibitors of the enzyme estrone sulfatase (ES). The results of the study show that these compounds are potent inhibitors, possessing greater inhibitory activity than COUMATE, but weaker inhibitory activity than EMATE or the tricyclic derivative of COUMATE, namely 667-COUMATE. Furthermore, the compounds are observed to be irreversible inhibitors.

Item Type: Article
Uncontrolled Keywords: nonsteroidal 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: Automatic Import Agent
Date Deposited: 10 Mar 2010 16:06
Last Modified: 19 Nov 2010 14:49
URI: http://eprints.kingston.ac.uk/id/eprint/7200

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