Novel tricyclic inhibitors of IKK2: discovery and SAR leading to the identification of 2-methoxy-N-((6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl)pyridin-2-yl)methyl)acetamide (BMS-066).
Bioorg Med Chem Lett
; 21(23): 7006-12, 2011 Dec 01.
Article
en En
| MEDLINE
| ID: mdl-22018461
ABSTRACT
The synthesis, structure-activity relationships (SAR), and biological results of pyridyl-substituted azaindole based tricyclic inhibitors of IKK2 are described. Compound 4m demonstrated potent in vitro potency, acceptable pharmacokinetic and physicochemical properties, and efficacy when dosed orally in a mouse model of inflammatory bowel disease.
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Inhibidores Enzimáticos
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Quinasa I-kappa B
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Descubrimiento de Drogas
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Compuestos Heterocíclicos con 3 Anillos
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Acetamidas
Tipo de estudio:
Diagnostic_studies
Límite:
Animals
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Humans
Idioma:
En
Año:
2011
Tipo del documento:
Article