First report of the investigation into the importance of pK[sub]a in the inhibition of estrone sulfatase by sulfamate containing compounds

Ahmed, Sabbir, James, Karen and Patel, Chirag K. (2000) First report of the investigation into the importance of pK[sub]a in the inhibition of estrone sulfatase by sulfamate containing compounds. Biochemical and Biophysical Research Communications, 272(2), pp. 583-585. ISSN (print) 0006-291X

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Abstract

In an effort to rationalise the inhibitory activity of a range of aminosulfamate compounds and to further investigate the recently reported definitive pharmacophore estrone sulfatase (ES), we undertook extensive synthesis, biochemical evaluation and physicochemical property determination of a range of similar compounds. Here, we report the initial results of our study into a series of simple (aminosulfonate based) substituted phenol derivatives. Using these compounds, we investigated the role of pK(a) in the inhibition of ES. The results of the study suggest that there is a strong correlation between the inhibitory activity and the stability of the resulting O(-) anion (i.e., the pK(a) of the starting phenol).

Item Type: Article
Uncontrolled Keywords: aromatase inhibitors, steroid sulfatase, breast-cancer
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: 16 Mar 2010 08:25
Last Modified: 14 Apr 2011 12:14
URI: http://eprints.kingston.ac.uk/id/eprint/7245

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