Login

Journal Image
Letters in Drug Design & Discovery
ISSN (Print): 1570-1808
ISSN (Online): 1875-628X
VOLUME: 11
ISSUE: 8
DOI: 10.2174/1570180811666131230235538      Price:  $58









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

img
Author(s): Pallav S. Shah, Imran Shahid, Wai-Yee Lee, Caroline P. Owen and Sabbir Ahmed
Pages 1000-1009 (10)
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.
Graphical Abstract:
Keywords:
17α-hydroxylase/17, 17α-OHase, 20-lyase, Azole, Inhibitors Lyase.
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.