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 3,5- Dibromo Derivatives of 4-Hydroxyphenyl Ketone-Based Compounds as Probes of the Active Site of Type 3 of 17β-Hydroxysteroid Dehydrogenase (17β-HSD3) and the Role of Hydrogen Bonding Interaction in the Inhibition of 17β-HSD3

Author(s): Moniola S. Olusanjo, Shreena N. Mashru, Timothy Cartledge, Sabbir Ahmed.

Abstract:

We report the synthesis, evaluation and rationalisation of the inhibitory activity of a series of 3,5-dibromo derivatives of 4-hydroxyphenyl ketone as probes of the active site of the type 3 of 17β-hydroxysteroid dehydrogenase (17β-HSD3). The results support the important role of hydrogen bonding interaction in the inhibition of 17β-HSD3.

Keywords: Androgen ablation, Enzyme inhibition, Hydrogen bonding, 17β-hydroxysteroid dehydrogenase, Type 3

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Article Details

VOLUME: 9
ISSUE: 6
Year: 2012
Page: [604 - 610]
Pages: 7
DOI: 10.2174/157018012800672994
Price: $58