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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.