Synthesis and structure-activity relationships of 1,2,4-triazolo[1,5-a]pyrimidin-7(3H)-ones as novel series of potent ß isoform selective phosphatidylinositol 3-kinase inhibitors.
Bioorg Med Chem Lett
; 22(9): 3198-202, 2012 May 01.
Article
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| MEDLINE
| ID: mdl-22475557
ABSTRACT
A series of 1,2,4-triazolo[1,5-a]pyrimidin-7(3H)-ones with excellent enzyme inhibition, improved isoform selectivity, and excellent inhibition of downstream phosphorylation of AKT has been identified. Several compounds in the series demonstrated potent (â¼ 0.100 µM IC(50)) growth inhibition in a PTEN deficient cancer cell line.
Texto completo:
1
Bases de datos:
MEDLINE
Asunto principal:
Inhibidores de Proteínas Quinasas
/
Inhibidores de las Quinasa Fosfoinosítidos-3
Límite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2012
Tipo del documento:
Article
País de afiliación:
Estados Unidos