4.5 Article

Synthesis and biochemical evaluation of a range of sulfonated derivatives of 4-hydroxybenzyl imidazole as highly potent inhibitors of rat testicular 17α-hydroxylase/17,20-lyase (P-45017α)

期刊

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 16, 页码 4698-4701

出版社

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.06.070

关键词

Hydroxylase; Lyase; Prostate cancer; Inhibition; Sulfonate

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We report the synthesis and biochemical evaluation of a range of 4-sulfonated derivatives of 4-hydroxybenzyl imidazole which has been targetted against the two components of 17 alpha-hydroxylase/17,20-lyase (P-450(17 alpha)), namely, 17 alpha-hydroxylase (17 alpha-OHase) and 17,20-lyase (lyase). The results from the biochemical testing suggest that the compounds synthesised are highly potent inhibitors possessing excellent selectivity towards the lyase component. (C) 2009 Elsevier Ltd. All rights reserved.

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