硫代磷酸盐
甾体硫酸酯酶
化学
磷酸盐
类固醇
药理学
生物化学
苯乙胺类
联苯
立体化学
生物
有机化学
激素
作者
Sebastian Demkowicz,Witold Kozak,Mateusz Daśko,Maciej Masłyk,Konrad Kubiński,Janusz Rachoń
摘要
Preclinical Research In the present work, we report convenient methods for the synthesis and biological evaluation of phosphate and thiophosphate biphenyl derivatives exhibiting steroid sulfatase (STS) activity. The described synthesis is based on straightforward preparation of biphenyl-4-ol and 4′-hydroxy-biphenyl-4-carboxylic acid ethyl ester modified with various phosphate or thiophosphate moieties. The inhibitory effects of these compounds were tested on STS isolated from human placenta and led to two compounds of interest, 5a and 5d with IC50 values of 28.0 and 22.1 µM, respectively and that had interesting new binding modes in the STS active site. Drug Dev Res 76 : 8294–104, 2015. © 2015 Wiley Periodicals, Inc.
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