Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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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

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

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.

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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Article Details

VOLUME: 9
ISSUE: 1
Year: 2012
Page: [69 - 76]
Pages: 8
DOI: 10.2174/157018012798193044