Environmental Health Science Laboratory, Sumitomo Chemical Co., Ltd, 1-98, Kasugadenaka 3-chome, Konohana-ku, Osaka 554-8558, Japan.
Bioorg Med Chem Lett. 2012 Jan 1;22(1):504-7. doi: 10.1016/j.bmcl.2011.10.095. Epub 2011 Nov 12.
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.
基于噁唑烷二酮和噻唑烷二酮衍生物，我们从高通量筛选命中物 5-(3-溴-4-羟基苄基)-3-(4-甲氧基苯基)-1,3-噻唑-2-酮中鉴定出新型强效 17β-羟甾脱氢酶 3（17β-HSD3）抑制剂。5-(3-溴-4-羟基苯亚甲基)-3-(4-甲氧基苯基)-2-硫代-1,3-噻唑烷-4-酮表现出有前景的活性概况，并对相关的 17β-HSD 同工酶和核受体表现出显著的选择性。
