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

Ahmed, Sabbir, James, Karen and Owen, Caroline P. (2002) Design, synthesis and biochemical evaluation of AC ring mimics as novel inhibitors of the enzyme estrone sulfatase (ES). The Journal of Steroid Biochemistry and Molecular Biology, 82(4-5), pp. 425-435. ISSN (print) 0960-0760

Full text not available from this archive.

Abstract

We report the results of our study into a series of 4'-O-sulfamoyl-4-biphenyl based compounds as novel inhibitors of the enzyme estrone sulfatase (ES). From the results of the molecular modeling design process, it was suggested that these compounds would be able to mimic both the A and C rings of the steroid backbone, and thus possess inhibitory activity against ES. The results of the biochemical evaluation study show that these compounds are indeed good 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: estrone sulfatase, emate, coumate, steroid sulfatase, nonsteroidal inhibitors, potent inhibitors, estrone-3-o-sulfamate
Research Area: Chemistry
Faculty, School or Research Centre: Faculty of Science (until 2011) > School of Pharmacy and Chemistry
Related URLs:
Depositing User: Automatic Import Agent
Date Deposited: 10 Mar 2010 14:18
Last Modified: 14 Apr 2011 12:01
URI: http://eprints.kingston.ac.uk/id/eprint/7182

Actions (Repository Editors)

Item Control Page Item Control Page