| Autor: |
Bernotas RC; Chemical and Screening Sciences, Wyeth Pharmaceuticals, 500 Arcola Road, Collegeville, PA 19426, USA. bernotr@wyeth.com, Singhaus RR, Kaufman DH, Ullrich J, Fletcher H 3rd, Quinet E, Nambi P, Unwalla R, Wilhelmsson A, Goos-Nilsson A, Farnegardh M, Wrobel J |
| Jazyk: |
angličtina |
| Zdroj: |
Bioorganic & medicinal chemistry [Bioorg Med Chem] 2009 Feb 15; Vol. 17 (4), pp. 1663-70. Date of Electronic Publication: 2008 Dec 27. |
| DOI: |
10.1016/j.bmc.2008.12.048 |
| Abstrakt: |
A series of 4-(amido-biarylether)-quinolines was prepared as potential LXR agonists. Appropriate substitution with amide groups provided high affinity LXR ligands, some with excellent potency and efficacy in functional assays of LXR activity. Novel amide 4g had a binding IC(50)=1.9 nM for LXRbeta and EC(50)=34 nM (96% efficacy relative to T0901317) in an ABCA1 gene expression assay in mouse J774 cells, demonstrating that 4-(biarylether)-quinolines with appropriate amide substitution are potent LXR agonists. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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