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
Letters in Drug Design & Discovery
Title: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
Volume: 9 Issue: 6
Author(s): Moniola S. Olusanjo, Shreena N. Mashru, Timothy Cartledge and Sabbir Ahmed
Affiliation:
Keywords: Androgen ablation, Enzyme inhibition, Hydrogen bonding, 17β-hydroxysteroid dehydrogenase, Type 3
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.
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S. Olusanjo Moniola, N. Mashru Shreena, Cartledge Timothy and Ahmed Sabbir, 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, Letters in Drug Design & Discovery 2012; 9 (6) . https://dx.doi.org/10.2174/157018012800672994
DOI https://dx.doi.org/10.2174/157018012800672994 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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