Synthesis and evaluation of novel 3,4,6-substituted 2-quinolones as FMS kinase inhibitors.
Bioorg Med Chem Lett
; 18(6): 2097-102, 2008 Mar 15.
Article
em En
| MEDLINE
| ID: mdl-18289848
ABSTRACT
A series of 3,4,6-substituted 2-quinolones has been synthesized and evaluated as inhibitors of the kinase domain of macrophage colony-stimulating factor-1 receptor (FMS). The fully optimized compound, 4-(4-ethyl-phenyl)-3-(2-methyl-3H-imidazol-4-yl)-2-quinolone-6-carbonitrile 21b, has an IC(50) of 2.5 nM in an in vitro assay and 5.0 nM in a bone marrow-derived macrophage cellular assay. Inhibition of FMS signaling in vivo was also demonstrated in a mouse pharmacodynamic model.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Receptor de Fator Estimulador de Colônias de Macrófagos
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Quinolonas
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Inibidores de Proteínas Quinases
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Macrófagos
Tipo de estudo:
Evaluation_studies
/
Prognostic_studies
Limite:
Animals
Idioma:
En
Ano de publicação:
2008
Tipo de documento:
Article