2-Benzimidazolyl-9-(chroman-4-yl)-purinone derivatives as JAK3 inhibitors.
Bioorg Med Chem Lett
; 19(23): 6788-92, 2009 Dec 01.
Article
in 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.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Purines
/
Benzimidazoles
/
Enzyme Inhibitors
/
Janus Kinase 3
Type of study:
Prognostic_studies
Limits:
Animals
Language:
En
Journal:
Bioorg Med Chem Lett
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2009
Document type:
Article
Affiliation country:
Estados Unidos