Identification of oxazolidinediones and thiazolidinediones as potent 17β-hydroxysteroid dehydrogenase type 3 inhibitors

K Harada, H Kubo, A Tanaka, K Nishioka

文献索引：Harada, Koichiro; Kubo, Hideki; Tanaka, Akio; Nishioka, Kazuhiko Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 1 p. 504 - 507

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被引用次数: 8

摘要

Novel and potent inhibitors of 17β-hydroxysteroid dehydrogenase type 3 (17β-HSD3) were identified based on oxazolidinedione and thiazolidinedione derivatives, starting from a high- throughput screening hit, 5-(3-bromo-4-hydroxybenzyl)-3-(4-methoxyphenyl)-1, 3-thiazol-2- one 1. 5-(3-Bromo-4-hydroxybenzylidene)-3-(4-methoxyphenyl)-2-thioxo-1, 3-thiazolidin-4- one 21 exhibited a promising activity profile and demonstrated significant selectivity over ...