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  • Title: First dual aromatase-steroid sulfatase inhibitors.
    Author: Woo LW, Sutcliffe OB, Bubert C, Grasso A, Chander SK, Purohit A, Reed MJ, Potter BV.
    Journal: J Med Chem; 2003 Jul 17; 46(15):3193-6. PubMed ID: 12852749.
    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 IC(50) 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.
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