Patel, Chirag K., Owen, Caroline P. and Ahmed, Sabbir (2004) Inhibition of estrone sulfatase (ES) by alkyl and cycloalkyl ester derivatives of 4-[(aminosulfonyl)oxy] benzoic acid. Bioorganic & Medicinal Chemistry Letters, 14(3), pp. 605-609. ISSN (print) 0960-894X
Official URL: http://dx.doi.org/doi:10.1016/j.bmcl.2003.11.067
Abstract
In our search for potent inhibitors of the enzyme estrone sulfatase (ES), we have undertaken the synthesis and biochemical evaluation of a range of esters of 4-[(aminosulfonyl)oxy] benzoic acid. The results of the study show that the synthesised compounds possess potent inhibitory activity, indeed the cyclooctyl derivative was found to be more potent than 667-COUMATE, which is currently undergoing clinical trials.
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