Letters in Drug Design & Discovery

Atta-ur-Rahman  , FRS
Honorary Life Fellow
Kings College
University of Cambridge
Cambridge
UK
Email: lddd@benthamscience.org

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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 and Sabbir Ahmed

Affiliation: Institute of Biomedical and Environmental Health Research (IBEHR), School of Science, Faculty of Science and Technology, University of the West of Scotland, Paisley, Renfrewshire, Scotland, PA1 2BE, UK.

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

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.

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Article Details

VOLUME: 11
ISSUE: 8
Page: [1000 - 1009]
Pages: 10
DOI: 10.2174/1570180811666131230235538