Non-hinge-binding pyrazolo[1,5-a]pyrimidines as potent B-Raf kinase inhibitors.
Bioorg Med Chem Lett
; 19(23): 6519-23, 2009 Dec 01.
Article
en En
| MEDLINE
| ID: mdl-19864136
ABSTRACT
As part of our research effort to discover B-Raf kinase inhibitors, we prepared a series of C-3 substituted N-(3-(pyrazolo[1,5-a]pyrimidin-7-yl)phenyl)-3-(trifluoromethyl)benzamides. X-ray crystallography studies revealed that one of the more potent inhibitors (10n) bound to B-Raf kinase without forming a hinge-binding hydrogen bond. With basic amine residues appended to C-3 aryl residues, cellular activity and solubility were enhanced over previously described compounds of this class.
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1
Banco de datos:
MEDLINE
Asunto principal:
Pirazoles
/
Pirimidinas
/
Benzamidas
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Proteínas Proto-Oncogénicas B-raf
/
Inhibidores de Proteínas Quinasas
Idioma:
En
Año:
2009
Tipo del documento:
Article