Carboxylic acid based quinolines as liver X receptor modulators that have LXRβ receptor binding selectivity

被引：31

作者：

Hu, Balhua ^{[1
]}

Quinet, Elaine ^{[3
]}

Unwalla, Rayomand ^{[1
]}

Collini, Mike ^{[1
]}

Jetter, James ^{[1
]}

Dooley, Rebecca ^{[1
]}

Andraka, Diane ^{[1
]}

Nogle, Lisa ^{[1
]}

Savio, Dawn ^{[3
]}

Halpern, Anita ^{[3
]}

Goos-Nilsson, Annika ^{[2
]}

Wilhelmsson, Anna ^{[2
]}

Nambi, Ponnal ^{[3
]}

Wrobel, Jay ^{[1
]}

机构：

[1] Wyeth Pharmaceut, Chem & Screening Sci, Collegeville, PA 19426 USA

[2] Karo Bio, Huddinge, Sweden

[3] Wyeth Pharmaceut, Cardiovasc & Metab Dis, Collegeville, PA 19426 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 01期

关键词：

LXR agonists; selectivity in binding assays; quinolines; carboxylic acids;

D O I：

10.1016/j.bmcl.2007.11.013

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of potent and binding selective LXR beta agonists was developed using the previously reported non-selective LXR ligand WAY-254011 as a structural template. With the aid of molecular modeling, it was found that 2,3-diMe-Ph, 2,5-diMe-Ph, and naphthalene substituted quinoline acetic acids (such as quinoline 33, 37, and 38) showed selectivity for LXR beta over LXR alpha in binding assays. (C) 2007 Elsevier Ltd. All rights reserved.

引用

页码：54 / 59

页数：6

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