Lota Rupinder K, Dhanani Sachin, Owen Caroline P, Ahmed Sabbir
Department of Pharmacy, School of Pharmacy and Chemistry, Kingston University, Kingston upon Thames, Surrey, UK.
Bioorg Med Chem Lett. 2006 Sep 1;16(17):4519-22. doi: 10.1016/j.bmcl.2006.06.029. Epub 2006 Jun 22.
We report the preliminary results of the synthesis and biochemical evaluation of a number of 4-hydroxyphenyl ketones as inhibitors of the isozyme of the enzyme 17beta-hydroxysteroid dehydrogenase (17beta-HSD) responsible for the conversion of androstenedione (AD) to testosterone (T), more specifically type 3 (17beta-HSD3). The results of our study suggest that we have synthesised compounds which are, in general, potent inhibitors of 17beta-HSD3, in particular, we discovered that 1-(4-hydroxy-phenyl)-nonan-1-one (8) was the most potent (IC(50) = 2.86 +/- 0.03 microM). We have therefore provided good lead compounds in the synthesis of novel non-steroidal inhibitors of 17beta-HSD3.
我们报告了一系列4-羟基苯酮作为17β-羟基类固醇脱氢酶（17β-HSD）同工酶抑制剂的合成及生化评估的初步结果，该同工酶负责将雄烯二酮（AD）转化为睾酮（T），更具体地说是3型（17β-HSD3）。我们的研究结果表明，我们合成的化合物总体上是17β-HSD3的有效抑制剂，特别是我们发现1-（4-羟基苯基）壬-1-酮（8）是最有效的（IC50 = 2.86 +/- 0.03 microM）。因此，我们在新型17β-HSD3非甾体抑制剂的合成中提供了良好的先导化合物。
