Acid dissociation constant, a potential physicochemical factor in the inhibition of the enzyme estrone sulfatase (ES)

Ahmed, Sabbir, Owen, Caroline P., James, Karen, Patel, Chirag K. and Patel, Mijal (2001) Acid dissociation constant, a potential physicochemical factor in the inhibition of the enzyme estrone sulfatase (ES). Bioorganic & Medicinal Chemistry Letters, 11(7), pp. 899-902. ISSN (print) 0960-894X

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Abstract

We report the initial results of the synthesis and biochemical evaluation of a series of aminosulfonate based compounds of phenol and the determination of the pKa of the parent phenol in an attempt to investigate the role of this physicochemical factor in the irreversible inhibition of the enzyme estrone sulfatase (ES). The results of the study show that there is a strong correlation between the observed pKa and inhibitory activity. We postulate that the stability of the phenoxide ion, as indicated by the acid dissociation constant, is an important factor in the irreversible inhibition of this enzyme.

Item Type: Article
Uncontrolled Keywords: steroid sulfatase, analogs
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: 27 Apr 2011 15:31
URI: http://eprints.kingston.ac.uk/id/eprint/1381

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