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)

被引：10

作者：

Ahmed, Sabbir ^{[1
]}

Shahid, Imran ^{[2
]}

Dhanani, Sachin ^{[1
]}

Owen, Caroline P. ^{[1
]}

机构：

[1] Univ W Scotland, Sch Sci, Paisley PA1 2BE, Renfrew, Scotland

[2] Kingston Univ, Sch Pharm & Chem, Kingston KT1 2EE, Surrey, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 16期

关键词：

Hydroxylase; Lyase; Prostate cancer; Inhibition; Sulfonate; P450(17-ALPHA); CANCER; RATIONALIZATION; CHEMOTHERAPY; AROMATASE; TARGET;

D O I：

10.1016/j.bmcl.2009.06.070

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

页码：4698 / 4701

页数：4

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