Synthesis and structure-activity relationships of potent retinoid X receptor ligands

被引：14

作者：

Farmer, LJ

Jeong, S

Kallel, EA

Koch, SSC

Croston, GE

Flatten, KS

Heyman, RA

Nadzan, AM

机构：

[1] LIGAND PHARMACEUT INC,DEPT NEW LEADS,SAN DIEGO,CA 92121

[2] LIGAND PHARMACEUT INC,DEPT ENDOCRINE RES,SAN DIEGO,CA 92121

[3] LIGAND PHARMACEUT INC,DEPT RETINOID RES,SAN DIEGO,CA 92121

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 18期

关键词：

D O I：

10.1016/S0960-894X(97)00437-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of potent retinoid X receptor (RXR) selective ligands was designed and prepared. The lead compound 7a showed good binding (K-i; 20-50 nM) and transactivation (EC50; 40-50 nM) to the RXR subfamily of retinoid receptors. More importantly, small variations in the geometry of the cyclopentane ring moiety led to 9, one of the most potent RXR agonists to date (K-i: 3-8 nM; EC50: 3-4 nM). (C) 1997 Elsevier Science Ltd.

引用

页码：2393 / 2398

页数：6

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