Discovery of potent and selective PKC-theta inhibitors.
Bioorg Med Chem Lett
; 17(1): 225-30, 2007 Jan 01.
Article
en En
| MEDLINE
| ID: mdl-17055721
ABSTRACT
An uHTS campaign was performed to identify selective inhibitors of PKC-theta. Initial triaging of the hit set based on selectivity and historical analysis led to the identification of 2,4-diamino-5-nitropyrimidines as potent and selective PKC-theta inhibitors. A homology model and initial SAR is presented demonstrating that a 2-arylalkylamino substituent in conjunction with suitable 4-diamino substituent are essential for achieving selectivity over many kinases. Additional hit to lead profiling is presented on selected compounds.
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Bases de datos:
MEDLINE
Asunto principal:
Pirimidinas
/
Proteína Quinasa C
/
Inhibidores de Proteínas Quinasas
/
Isoenzimas
Tipo de estudio:
Prognostic_studies
Límite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2007
Tipo del documento:
Article
País de afiliación:
Estados Unidos