Discovery of potent and orally bioavailable 17β-hydroxysteroid dehydrogenase type 3 inhibitors

…, A Conception, S Inoue, S Okada, K Nishioka

Index: Harada, Koichiro; Kubo, Hideki; Abe, Jun; Haneta, Mari; Conception, Arnel; Inoue, Shinichi; Okada, Satoshi; Nishioka, Kazuhiko Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 10 p. 3242 - 3254

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Citation Number: 2

Abstract

We have previously reported the discovery of a new class of potent inhibitors of 17β- hydroxysteroid dehydrogenase type 3 (17β-HSD3) derived from benzylidene oxazolidinedione and thiazolidinedione scaffolds. In this study, these analogs were designed, synthesized, and evaluated in a human cell-based assay. The detailed structure– activity relationship (SAR) surrounding this pharmacophore were developed, and ...