Synthesis of 4-(3-biaryl)quinoline sulfones as potent liver X receptor agonists.
Bioorg Med Chem Lett
; 20(9): 2903-7, 2010 May 01.
Article
en En
| MEDLINE
| ID: mdl-20382019
ABSTRACT
A series of 4-(3-biaryl)quinolines with sulfone substituents on the terminal aryl ring (8) was prepared as potential LXR agonists. High affinity LXRbeta ligands with generally modest binding selectivity over LXRalpha and excellent agonist potency in LXR functional assays were identified. Many compounds had LXRbeta binding IC(50) values <10 nM while the most potent had EC(50) values <1.0 nM in an ABCA1 mRNA induction assay in J774 mouse cells with efficacy comparable to T0901317. Sulfone 8a was further evaluated in LDL (-/-) mice and shown to reduce atherosclerotic lesion progression.
Texto completo:
1
Base de datos:
MEDLINE
Asunto principal:
Quinolinas
/
Sulfonas
/
Receptores Nucleares Huérfanos
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2010
Tipo del documento:
Article
País de afiliación:
Estados Unidos