Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1377706 | Bioorganic & Medicinal Chemistry Letters | 2006 | 4 Pages |
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 17β-hydroxysteroid dehydrogenase (17β-HSD) responsible for the conversion of androstenedione (AD) to testosterone (T), more specifically type 3 (17β-HSD3). The results of our study suggest that we have synthesised compounds which are, in general, potent inhibitors of 17β-HSD3, in particular, we discovered that 1-(4-hydroxy-phenyl)-nonan-1-one (8) was the most potent (IC50 = 2.86 ± 0.03 μM). We have therefore provided good lead compounds in the synthesis of novel non-steroidal inhibitors of 17β-HSD3.
Graphical abstractWe report the preliminary results of the synthesis and biochemical evaluation of a number of novel inhibitors of type 3 isozyme of the enzyme 17β-hydroxysteroid dehydrogenase (17β-HSD3).Figure optionsDownload full-size imageDownload as PowerPoint slide