Anti-androgens with full antagonistic activity toward human prostate tumor LNCaP cells with mutated androgen receptor

被引：101

作者：

Ishioka, T ^{[1
]}

Tanatani, A ^{[1
]}

Nagasawa, K ^{[1
]}

Hashimoto, Y ^{[1
]}

机构：

[1] Univ Tokyo, Inst Mol & Cellular Biosci, Bunkyo Ku, Tokyo 1130032, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 16期

关键词：

D O I：

10.1016/S0960-894X(03)00575-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

Anti-androgens were designed based on the principle of inhibiting the folding of helix 12 of the nuclear androgen receptor. The prepared anti-androgens exhibited full antagonistic activity toward human prostate tumor LNCaP cells with T877A point-mutated nuclear androgen receptor, as far as examined, towards which other known anti-androgens, including hydroxyflutamide, are inactive or act as androgen agonists. (C) 2003 Elsevier Ltd. All rights reserved.

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页码：2655 / 2658

页数：4

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