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The 17beta-hydroxysteroid dehydrogenases (17beta-HSDs) catalyze the interconversion between the oxidized and reduced forms of androgens and estrogens at the 17 position. The 17beta-HSD type 1 enzyme (17beta-HSD1) catalyzes the reduction of estrone (E1) to estradiol and is expressed in malignant breast cells. Inhibitors of this enzyme thus have potential as treatments for hormone dependent breast cancer. Syntheses and biological evaluation of novel non-steroidal inhibitors designed to mimic the E1 template are reported using information from potent steroidal inhibitors. Of the templates investigated biphenyl ethanone was promising and led to inhibitors with IC(50) values in the low micromolar range.

Original publication

DOI

10.1016/j.bmc.2008.02.059

Type

Journal article

Journal

Bioorg Med Chem

Publication Date

15/04/2008

Volume

16

Pages

4438 - 4456

Keywords

17-Hydroxysteroid Dehydrogenases, Cell Line, Tumor, Drug Design, Enzyme Inhibitors, Humans, Molecular Structure, Structure-Activity Relationship