Synthesis, Biochemical Evaluation and Rationalisation of a Series of (3-O-Sulfonate) Derivatives of Estrone (E1) as Probes of the Active Site of Type 3 of the 17β-Hydroxysteroid Dehydrogenase (17β-HSD) Family of Enzymes

We report the use of sulfonate derivatives of estrone (E1) in the search for inhibitors of 17β-hydroxysteroid dehydrogenase, in particular, type 3 (17β-HSD3). Results suggest that the compounds are excellent inhibitors of 17β- HSD3 and a number were found to be extremely potent in comparison to the standard inhibitors used.