Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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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

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

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

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Article Details

VOLUME: 8
ISSUE: 3
Year: 2011
Page: [253 - 259]
Pages: 7
DOI: 10.2174/157018011794578259
Price: $58