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.
Keywords: Androgen ablation, 17β-hydroxysteroid dehydrogenase, steroid-based inhibitors, prostate cancer, type 3, Estrone (E1), 17β-Hydroxysteroid, 17β-Hsd, 17β-HSD3, hydride donor, NADPH, C(17)-OH, estradiol (E2), transition-states (TS), 13CNMR
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Published on: 01 March, 2012
Page: [69 - 76]