4-[3-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)phenyl]benzoic acid and heterocyclic-bridged analogues are novel retinoic acid receptor subtype and retinoid X receptor α agonists

被引：12

作者：

Dawson, MI

Jong, L

Hobbs, PD

Xiao, DM

Feng, KC

Chao, WR

Pan, C

Fontana, JA

Zhang, XK

机构：

[1] Mol Med Res Inst, Dept Med Chem, Mt View, CA 94043 USA

[2] SRI Int, Retinoid Program, Menlo Park, CA 94025 USA

[3] Burnham Inst, La Jolla, CA 92037 USA

[4] Wayne State Univ, John Dingell VA Med Ctr, Detroit, MI 48201 USA

[5] Wayne State Univ, Kamaros Canc Inst, Detroit, MI 48201 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 12期

关键词：

D O I：

10.1016/S0960-894X(00)00244-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Aromatic retinoids having a meta-substituted aromatic ring bridge, such as 4-[3-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)phenyl]benzoic acid and its 3,5-diaryl-substituted 4,5-dihydroisoxazole analogue, function as retinoid receptor panagonists by activating both retinoic acid and retinoid X receptors to induce gene transcription, and thereby provide novel scaffolds for retinoid drug development. Both classes of these ligand-inducible transcription factors are involved in mediating the inhibitory effects of retinoids on cancer cell growth. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：1311 / 1313

页数：3

共 16 条

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