N-Phenyl-N-purin-6-yl ureas: the design and synthesis of p38alpha MAP kinase inhibitors.
Bioorg Med Chem Lett
; 13(6): 1191-4, 2003 Mar 24.
Article
in En
| MEDLINE
| ID: mdl-12643941
ABSTRACT
The design, synthesis and SAR of a series of 2,6,9-trisubstituted purine inhibitors of p38alpha kinase is reported. Synthetic routes were devised to allow for array synthesis in which all three points of diversity could be facilely explored. The binding of this novel series to p38alpha kinase, which was predicted to have several key interactions in common with SB-203580, was confirmed by X-ray crystallography of 19 (p38 IC(50)=82 nM).
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Collection:
01-internacional
Database:
MEDLINE
Main subject:
Urea
/
Mitogen-Activated Protein Kinases
/
Enzyme Inhibitors
Type of study:
Prognostic_studies
Language:
En
Journal:
Bioorg Med Chem Lett
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2003
Type:
Article