Synthesis and Biochemical Evaluation of a Series of Methanesulfonate Derivatives of 4-Hydroxyphenyl Ketone as Probes of the Active Site of Type 3 OF 17β-Hydroxysteroid Dehydrogenase Family of Enzymes

We report the synthesis, evaluation and rationalisation of the inhibitory activity of a series of compounds as probes of the active site of the type 3 of 17β-hydroxysteroid dehydrogenase (17β-HSD3). Results have provided invaluable insight into the active site (as well as supporting the previously reported model) of 17β-HSD3.