2. Academic Validation
  3. Carboxylic acid based quinolines as liver X receptor modulators that have LXRbeta receptor binding selectivity

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

  • Bioorg Med Chem Lett. 2008 Jan 1;18(1):54-9. doi: 10.1016/j.bmcl.2007.11.013.
Baihua Hu 1,  Elaine Quinet,  Rayomand Unwalla,  Mike Collini,  James Jetter,  Rebecca Dooley,  Diane Andraka,  Lisa Nogle,  Dawn Savio,  Anita Halpern,  Annika Goos-Nilsson,  Anna Wilhelmsson,  Ponnal Nambi,  Jay Wrobel
Affiliations

Affiliation

  • 1 Chemical and Screening Sciences, Wyeth Pharmaceuticals, Collegeville, PA 19426, USA. hub@wyeth.com
PMID: 18023179 DOI: 10.1016/j.bmcl.2007.11.013
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.

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