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Letters in Drug Design & Discovery
ISSN (Print): 1570-1808
ISSN (Online): 1875-628X
Epub Full Text Article
DOI: 10.2174/1570180811666131230235538      Price:  $95

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
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; results 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.
17α-hydroxylase/17, 20-lyase, 17α-OHase, Lyase, Azole, Inhibitors
Institute of Biomedical and Environmental Health Reearch (IBEHR) School of Science Faculty of Science and Technology University of the West of Scotland Paisley, Renfrewshire Scotland PA1 2BE, UK Kingston University Kingston Surrey UK.