A new class of androgen receptor antagonists bearing carborane in place of a steroidal skeleton

被引：49

作者：

Fujii, S

Hashimoto, Y

Suzuki, T

Ohta, S

Endo, Y

机构：

[1] Tohoku Pharmaceut Univ, Fac Pharmaceut Sci, Aoba Ku, Sendai, Miyagi 9818558, Japan

[2] Tokushima Bunri Univ, Fac Pharmaceut Sci, Sanuki 7692193, Japan

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

[4] Hiroshima Univ, Grad Sch Med Sci, Minami Ku, Hiroshima 7348551, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 01期

关键词：

androgen antagonist; nuclear receptor; carborane; hydrophobic interaction;

D O I：

10.1016/j.bmcl.2004.09.091

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new class of androgen receptor antagonists containing dicarba-closo-dodecaborane (carborane) as a hydrophobic skeletal structure is described. The designed molecules bear the characteristic polar components of endogenous agonists, but have a hydrophobic carborane cage instead of the steroidal skeleton. These compounds bind to androgen receptor and show anti-androgenic activity towards androgen-dependent SC-3 cells with almost the same potency as the known anti-androgen hydroxyflutamide. (C) 2004 Elsevier Ltd. All rights reserved.

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页码：227 / 230

页数：4

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