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Synthesis, Biochemical Evaluation and Rationalisation of a Series of 3,5- Dibromo Derivatives of 4-Hydroxyphenyl Ketone-Based Compounds as Probes of the Active Site of Type 3 of 17β-Hydroxysteroid Dehydrogenase (17β-HSD3) and the Role of Hydrogen Bonding Interaction in the Inhibition of 17β-HSD3
Letters in Drug Design & Discovery ( IF 1.2 ) Pub Date : 2012-06-30 , DOI: 10.2174/157018012800672994
Moniola S. Olusanjo , Shreena N. Mashru , Timothy Cartledge , Sabbir Ahmed

We report the synthesis, evaluation and rationalisation of the inhibitory activity of a series of 3,5-dibromo derivatives of 4-hydroxyphenyl ketone as probes of the active site of the type 3 of 17β-hydroxysteroid dehydrogenase (17β-HSD3). The results support the important role of hydrogen bonding interaction in the inhibition of 17β-HSD3.



中文翻译:

一系列4-羟基苯基酮基化合物的3,5-二溴衍生物的合成,生化评估和合理化,作为17β-羟基类固醇脱氢酶(17β-HSD3)3型活性位点的探针以及氢键相互作用的作用在抑制17β-HSD3中

我们报告合成,评估和抑制活性的一系列4-羟基苯基酮的3,5-二溴衍生物作为17β-羟基类固醇脱氢酶(17β-HSD3)3型活性位点的探针。结果支持氢键相互作用在抑制17β-HSD3中的重要作用。

更新日期:2012-06-30
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