Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 49, Issue 21, Pages 6151-6154Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm0609566
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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 LXR beta and LXR alpha 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.
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