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
  • 1. Chemical and Screening Sciences, Wyeth Pharmaceuticals, Collegeville, PA 19426, USA. [email protected]
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.