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  • Title: Synthesis and biochemical evaluation of a range of (4-substituted phenyl)sulfonate derivatives of 4-hydroxybenzyl imidazole-based compounds as potent inhibitors of 17alpha-hydroxylase/17,20-lyase (P45017alpha) derived from rat testicular microsomes.
    Author: Owen CP, Shahid I, Lee WY, Ahmed S.
    Journal: Bioorg Med Chem Lett; 2010 Sep 01; 20(17):5345-8. PubMed ID: 20675132.
    Abstract:
    We report the synthesis, biochemical evaluation and rationalisation of the inhibitory activity of a range of (4-substituted phenyl)sulfonate derivatives of 4-hydroxybenzyl imidazole against the two components of 17alpha-hydroxylase/17,20-lyase (P450(17alpha)), namely, 17alpha-hydroxylase (17alpha-OHase) and 17,20-lyase (lyase). The results show the compounds to be highly potent inhibitors with limited selectivity towards the lyase component [e.g., toluene-4-sulfonic acid 4-imidazol-1-ylmethyl-phenyl ester (4) possessed an IC(50) value of 40 nM against 17alpha-OHase and 30 nM against lyase].
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