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

Title: 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

Volume: 8 Issue: 3

Author(s): Moniola S. Olusanjo, Timothy Cartledge, Kruti Shah and Sabbir Ahmed

Affiliation:

Keywords: Dual-inhibition, Enzyme inhibition, Hormone-dependent, 17β-hydroxysteroid dehydrogenase, Trifluoromethanesulfonate, Type 1, Type 3

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.

Cite this article as:

S. Olusanjo Moniola, Cartledge Timothy, Shah Kruti and Ahmed Sabbir, 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, Letters in Drug Design & Discovery 2011; 8 (3) . https://dx.doi.org/10.2174/157018011794578259