| Literature DB >> 17034119 |
Baihua Hu1, Michael Collini, Rayomand Unwalla, Christopher Miller, Robert Singhaus, Elaine Quinet, Dawn Savio, Anita Halpern, Michael Basso, James Keith, Valerie Clerin, Liang Chen, Christine Resmini, Qiang-Yuan Liu, Irene Feingold, Christine Huselton, Farooq Azam, Mathias Farnegardh, Cristofer Enroth, Tomas Bonn, Annika Goos-Nilsson, Anna Wilhelmsson, Ponnal Nambi, Jay Wrobel.
Abstract
A structure-based approach was used to optimize our new class of quinoline LXR modulators leading to phenyl acetic acid substituted quinolines 15 and 16. Both compounds displayed good binding affinity for LXRbeta and LXRalpha and were potent activators in LBD transactivation assays. The compounds also increased expression of ABCA1 and stimulated cholesterol efflux in THP-1 cells. Quinoline 16 showed good oral bioavailability and in vivo efficacy in a LDLr knockout mouse model for lesions.Entities:
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Year: 2006 PMID： 17034119 DOI： 10.1021/jm0609566
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446