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Bioorg Med Chem Lett. 2008 Jan 1;18(1):54-9. Epub 2007 Nov 9.

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

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1
Chemical and Screening Sciences, Wyeth Pharmaceuticals, Collegeville, PA 19426, USA. hub@wyeth.com

Abstract

A series of potent and binding selective LXRbeta 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 LXRbeta over LXRalpha in binding assays.

PMID:
18023179
DOI:
10.1016/j.bmcl.2007.11.013
[Indexed for MEDLINE]
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