Novel tricyclic inhibitors of IkappaB kinase.
J Med Chem
; 52(7): 1994-2005, 2009 Apr 09.
Article
in En
| MEDLINE
| ID: mdl-19267461
ABSTRACT
The design and synthesis of a novel series of oxazole-, thiazole-, and imidazole-based inhibitors of IkappaB kinase (IKK) are reported. Biological activity was improved compared to the pyrazolopurine lead, and the expedient synthesis of the new tricyclic systems allowed for efficient exploration of structure-activity relationships. This, combined with an iterative rat cassette dosing strategy, was used to identify compounds with improved pharmacokinetic (PK) profiles to advance for in vivo evaluation.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Oxazoles
/
Thiazoles
/
I-kappa B Kinase
/
Heterocyclic Compounds, 3-Ring
/
Imidazoles
Type of study:
Prognostic_studies
Limits:
Animals
/
Female
/
Humans
Language:
En
Journal:
J Med Chem
Journal subject:
QUIMICA
Year:
2009
Document type:
Article
Affiliation country:
United States