Synthesis and evaluation of novel 17-indazole androstene derivatives designed as CYP17 inhibitors

被引：46

作者：

Moreira, Vania M. A.

Vasaitis, Tadas S.

Njar, Vincent C. O.

Salvador, Jorge A. R.

机构：

[1] Univ Maryland, Sch Med, Dept Pharmacol & Expt Therapeut, Baltimore, MD 21201 USA

[2] Univ Coimbra, Fac Farm, Quim Farmaceut Lab, P-3000295 Coimbra, Portugal

来源：

STEROIDS | 2007年 / 72卷 / 14期

关键词：

indazole; CYP17; prostate cancer; androgen receptor; PC cell lines;

D O I：

10.1016/j.steroids.2007.08.004

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 [生物化学与分子生物学]; 081704 [应用化学];

摘要：

A series of novel 1H- and 2H-indazole derivatives of the commercially available dehydroepiandrosterone acetate have been synthesized and tested for inhibition of human cytochrome 17 alpha-hydroxylase-C-17,C-20-lyase (CYP17), androgen receptor (AR) binding affinity, and cytotoxic potential against three prostate cancer (PC) cell lines. (c) 2007 Elsevier Inc. All rights reserved.

引用

收藏

页码：939 / 948

页数：10

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