Letters in Drug Design & Discovery

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

Back

Synthesis and Biochemical Evaluation of a Range of 4-(n-alkanesulfonate) benzyl Imidazole-Based Compounds as Inhibitors of Rat Testicular 17α-hydroxylase/17,20-lyase (P45017α) in the Treatment of Hormone- Dependent Prostate Cancer

Author(s): Pallav S. Shah, Imran Shahid, Wai-Yee Lee, Caroline P. Owen, Sabbir Ahmed.

Graphical Abstract:


Abstract:

17α-Hydroxylase/17,20-lyase is a target in the treatment of hormone-dependent prostate cancer. Here we report the results of a study into a range of alkanesulfonate derivatives of 4-hydroxybenzylimidazole which show the compounds to be good inhibitors with 5 [IC50=1.11µM (17α-OHase) and IC50=1.28µM (lyase)] being the most potent but weaker than ketoconazole.

Keywords: 17α-hydroxylase/17, 17α-OHase, 20-lyase, Azole, Inhibitors Lyase.

Order Reprints Order Eprints Rights & PermissionsPrintExport

Article Details

VOLUME: 11
ISSUE: 8
Year: 2014
Page: [1000 - 1009]
Pages: 10
DOI: 10.2174/1570180811666131230235538
Price: $58