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

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-hydroxybenzy...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2012-01, Vol.22 (1), p.504-507
Hauptverfasser:	Harada, Koichiro, Kubo, Hideki, Tanaka, Akio, Nishioka, Kazuhiko
Format:	Artikel
Sprache:	eng
Schlagworte:	17-Hydroxysteroid Dehydrogenases - antagonists & inhibitors 17β-Hydroxysteroid dehydrogenase type 3 inhibitors Biological and medical sciences Carbon - chemistry Cell Nucleus - metabolism Chemistry, Pharmaceutical - methods Drug Design Enzyme Inhibitors - pharmacology Genes, Reporter HeLa Cells Humans Inhibitory Concentration 50 Isoenzymes - chemistry isozymes Male Medical sciences Models, Chemical Models, Molecular Molecular Conformation Oxazoles - chemical synthesis Oxazoles - pharmacology Oxazolidinedione Pharmacology. Drug treatments Prostate - chemistry Prostate cancer Prostatic Neoplasms - drug therapy receptors screening Thiazolidinedione thiazolidinediones Thiazolidinediones - chemical synthesis Thiazolidinediones - pharmacology
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Beschreibung
Zusammenfassung:	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 the related 17β-HSD isoenzymes and nuclear receptors.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2011.10.095