Synthesis and Biochemical Evaluation of a Series of Trifluoromethanesulfonate Derivatives of 4 Hydroxyphenyl Ketones – Probes of the Active Site of Type 1 and 3 of the 17β-Hydroxysteroid Dehydrogenase Family of Enzymes
Moniola S. Olusanjo,
In an effort to aid the design of ‘dual-inhibitors’ of types 1 and 3 of the 17β-hydroxysteroid dehydrogenase (17β-HSD), we report the synthesis, biochemical evaluation and rationalisation of the inhibitory activity of trifluoromethanesulfonate derivatives of 4-hydroxyphenyl ketone-based compounds which were found to be weak inhibitors of types 1 and 3.
Keywords: Dual-inhibition, Enzyme inhibition, Hormone-dependent, 17β-hydroxysteroid dehydrogenase, Trifluoromethanesulfonate, Type 1, Type 3
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