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

Title: 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

Volume: 9 Issue: 1

Author(s): Mohsen Akbarzadeh, Moniola S. Olusanjo and Sabbir Ahmed

Affiliation:

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

Abstract: 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.

Cite this article as:

Akbarzadeh Mohsen, S. Olusanjo Moniola and Ahmed Sabbir, 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, Letters in Drug Design & Discovery 2012; 9 (1) . https://dx.doi.org/10.2174/157018012798193044

DOI https://dx.doi.org/10.2174/157018012798193044	Print ISSN 1570-1808
Publisher Name Bentham Science Publisher	Online ISSN 1875-628X