Tricyclic azepine derivatives: pyrimido[4,5-b]-1,4-benzoxazepines as a novel class of epidermal growth factor receptor kinase inhibitors.
Bioorg Med Chem Lett
; 16(6): 1643-6, 2006 Mar 15.
Article
em En
| MEDLINE
| ID: mdl-16412636
ABSTRACT
A novel class of pyrimido[4,5-b]-1,4-benzoxazepines is described as inhibitors of epidermal growth factor receptor (EGFR) tyrosine kinase. Two compounds display potent EGFR inhibitory activity of less than 1 microM in cellular phosphorylation assays (IC(50) 0.47-0.69 microM) and are highly selective against a small kinase panel. Such compounds demonstrate anti-EGFR activity within a class that is different from any known EGFR inhibitor scaffolds. They also provide a basis for the design of kinase inhibitors with the desired selectivity profile.
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Base de dados:
MEDLINE
Assunto principal:
Azepinas
/
Inibidores de Proteínas Quinases
/
Receptores ErbB
Idioma:
En
Ano de publicação:
2006
Tipo de documento:
Article