Abstract
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