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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

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

Volume 11, Issue 8, 2014

Page: [1000 - 1009] Pages: 10

DOI: 10.2174/1570180811666131230235538

Price: $65

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.

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