Imidazo[1,5-a]quinoxalines as irreversible BTK inhibitors for the treatment of rheumatoid arthritis.
Bioorg Med Chem Lett
; 21(21): 6258-63, 2011 Nov 01.
Article
em En
| MEDLINE
| ID: mdl-21958547
ABSTRACT
Imidazo[1,5-a]quinoxalines were synthesized that function as irreversible Bruton's tyrosine kinase (BTK) inhibitors. The syntheses and SAR of this series of compounds are presented as well as the X-ray crystal structure of the lead compound 36 in complex with a gate-keeper variant of ITK enzyme. The lead compound showed good in vivo efficacy in preclinical RA models.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Artrite Reumatoide
/
Quinoxalinas
/
Proteínas Tirosina Quinases
/
Inibidores de Proteínas Quinases
Limite:
Humans
Idioma:
En
Ano de publicação:
2011
Tipo de documento:
Article