Synthesis and Biological Evaluation of 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1) Inhibitors Based on a Thieno [2, 3-d] pyrimidin-4 (3 H)-one Core

…, S Alho-Richmond, P Koskimies…

Index: Lilienkampf, Annamaria; Karkola, Sampo; Alho-Richmond, Sari; Koskimies, Pasi; Johansson, Nina; Huhtinen, Kaisa; Vihko, Kimmo; Waehaelae, Kristiina Journal of Medicinal Chemistry, 2009 , vol. 52, # 21 p. 6660 - 6671

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Citation Number: 32

Abstract

Many breast tumors are hormone-dependent, and estrogens, especially estradiol (E2), have a pivotal role in their growth and development. 17β-Hydroxysteroid dehydrogenase type 1 (17β-HSD1) is a key enzyme in the biosynthesis of female sex steroids, catalyzing the NADPH-dependent reduction of estrone into biologically active estradiol. In this study, a library of fused (di) cycloalkeno thieno [2, 3-d] pyrimidin-4 (3 H)-one based compounds ...