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

  • Bioorg Med Chem Lett. 2012 Jan 1;22(1):504-7. doi: 10.1016/j.bmcl.2011.10.095.
Koichiro Harada  1 ,  Hideki Kubo ,  Akio Tanaka ,  Kazuhiko Nishioka
Affiliations
  • 1. Environmental Health Science Laboratory, Sumitomo Chemical Co., Ltd, 1-98, Kasugadenaka 3-chome, Konohana-ku, Osaka 554-8558, Japan. [email protected]
PMID: 22137341 DOI: 10.1016/j.bmcl.2011.10.095
Abstract

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. 5-(3-Bromo-4-hydroxybenzylidene)-3-(4-methoxyphenyl)-2-thioxo-1,3-thiazolidin-4-one exhibited a promising activity profile and demonstrated significant selectivity over the related 17β-HSD isoenzymes and nuclear receptors.

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