2-Benzimidazolyl-9-(chroman-4-yl)-purinone derivatives as JAK3 inhibitors.
Bioorg Med Chem Lett
; 19(23): 6788-92, 2009 Dec 01.
Article
em En
| MEDLINE
| ID: mdl-19836234
ABSTRACT
A novel class of Janus tyrosine kinase 3 (JAK3) inhibitors based on a 2-benzimidazoylpurinone core structure is described. Through substitution of the benzimidazoyl moiety and optimization of the N-9 substituent of the purinone, compound 24 was identified incorporating a chroman-based functional group. Compound 24 shows excellent kinase activity, good oral bioavailability and demonstrates efficacy in an acute mechanistic mouse model through inhibition of interleukin-2 (IL-2) induced interferon-gamma (INF-gamma) production.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Purinas
/
Benzimidazóis
/
Inibidores Enzimáticos
/
Janus Quinase 3
Tipo de estudo:
Prognostic_studies
Limite:
Animals
Idioma:
En
Revista:
Bioorg Med Chem Lett
Ano de publicação:
2009
Tipo de documento:
Article