Synthesis and biological evaluation of (6-and 7-Phenyl) coumarin derivatives as selective nonsteroidal inhibitors of 17β-hydroxysteroid dehydrogenase type 1

…, J Cesar, T Lanišnik Rižner, S Gobec

Index: Starcevic, Stefan; Brozic, Petra; Turk, Samo; Cesar, Jozko; Lanisnik Rizner, Tea; Gobec, Stanislav Journal of Medicinal Chemistry, 2011 , vol. 54, # 1 p. 248 - 261

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Citation Number: 33

Abstract

17β-Hydroxysteroid dehydrogenase type 1 (17β-HSD1) is an enzyme that catalyzes NADPH- dependent reduction of the weak estrogen, estrone, into the most potent estrogen, estradiol, which exerts proliferative effects via the estrogen receptors. Overexpression of 17β-HSD1 in estrogen-responsive tissues is related to the development of hormone-dependent diseases, such as breast cancer and endometriosis; thus, 17β-HSD1 represents an attractive target ...