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
Moniola S. Olusanjo,
Shreena N. Mashru,
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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