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The Strathprints institutional repository is a digital archive of University of Strathclyde research outputs. Strathprints provides access to thousands of Open Access research papers by University of Strathclyde researchers, including those from the School of Psychological Sciences & Health - but also papers by researchers based within the Faculties of Science, Engineering, Humanities & Social Sciences, and from the Strathclyde Business School.

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First dual aromatase-steroid sulfatase inhibitors

Woo, L.W.L. and Sutcliffe, O.B. and Bubert, C. and Grasso, A. and Chander, S.K. and Purohit, A. and Reed, M.J. and Potter, B.V.L. (2003) First dual aromatase-steroid sulfatase inhibitors. Journal of Medicinal Chemistry, 46 (15). pp. 3193-3196. ISSN 0022-2623

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Abstract

Aromatase inhibitors in clinical use block the biosynthesis of estrogens. Hydrolysis of estrone 3-sulfate by steroid sulfatase is an important additional source of tumor estrogen, and blockade of both enzymes should provide a more effective endocrine therapy. Sulfamoylated derivatives of the aromatase inhibitor YM511 inhibited sulfatase and aromatase in JEG-3 cells with respective IC50 values of 20-227 and 0.82-100 nM (cf. letrozole, 0.89 nM). One dual inhibitor was potent against both enzymes in vivo, validating the concept.