Novel inhibitors of 17β-hydroxysteroid dehydrogenase type 1: Templates for design

…, M Huchet, E Ferrandis, MJ Reed, A Purohit…

Index: Allan, Gillian M.; Vicker, Nigel; Lawrence, Harshani R.; Tutill, Helena J.; Day, Joanna M.; Huchet, Marion; Ferrandis, Eric; Reed, Michael J.; Purohit, Atul; Potter, Barry V.L. Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 8 p. 4438 - 4456

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Citation Number: 44

Abstract

The 17β-hydroxysteroid dehydrogenases (17β-HSDs) catalyze the interconversion between the oxidized and reduced forms of androgens and estrogens at the 17 position. The 17β- HSD type 1 enzyme (17β-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 ...