Diarylamines Incorporating Hexahydrophenalene or Octahydrobenzoheptalene as Retinoid X Receptor (RXR)-Specific Agonists

被引：5
|
作者：
Amano, Yohei [1 ]
Noguchi, Masayuki [1 ]
Shudo, Koichi [1 ]
机构：
[1] Res Fdn ITSUU Lab, Setagaya Ku, Tokyo 1580094, Japan
来源：
CHEMICAL & PHARMACEUTICAL BULLETIN | 2014年 / 62卷 / 03期
关键词：
retinoid; retinoic acid receptor; retinoid X receptor (RXR); RXR-specific ligand; UNION-OF-PHARMACOLOGY; ALZHEIMERS-DISEASE; DESIGN; ACID;
D O I：
10.1248/cpb.c13-00740
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Selective ligands for retinoic acid receptors (RARs) and for retinoid X receptors (RXRs) are required for both biological studies and therapeutic purposes. We have synthesized a series of diarylamines incorporating hexahydrophenalene or octahydrobenzoheptalene as a hydrophobic moiety and examined their activities towards RARs and RXRs. Most of these compounds showed agonistic activity towards RXRs, but were inactive towards RARs. These RXR-specific ligands showed synergistic activity in RAR alpha,beta ligand-induced terminal differentiation of leukemia cell line HL-60.
引用
收藏
页码：254 / 259
页数：6
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