Phenylcyclohexene and phenylcyclohexadiene substituted compounds having retinoid antagonist activity

被引：11

作者：

Beard, RL

Klein, ES

Standeven, AM

Escobar, M

Chandraratna, RAS ^{[1
]}

机构：

[1] Allergan Pharmaceut Inc, Retinoid Res, Dept Chem, Irvine, CA 92623 USA

[2] Allergan Pharmaceut Inc, Retinoid Res, Dept Biol, Irvine, CA 92623 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 06期

关键词：

D O I：

10.1016/S0960-894X(01)00058-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Retinoids are natural and synthetic analogues of the hormone retinoic acid. Systemic retinoid agonist therapy is usually associated with toxic side effects, such as mucocutaneous toxicity, which may be alleviated by the use of topical retinoid antagonists. We report the synthesis and biological activity of a new series of potent, RAR-specific antagonists substituted with phenyl cyclohexene and phenylcyclohexadiene groups. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：765 / 768

页数：4

共 22 条

[1]

AGNISH ND, 1992, RETINOIDS CLIN PRACT, P47

[2]

ALLEGRETTO EA, 1993, J BIOL CHEM, V268, P26625

[3]

ALLERGAN INC, 1998, Patent No. 5760276

[4]

CHANDRARATNA RAS, 1988, Patent No. 4739098