Development of isoform selective PI3-kinase inhibitors as pharmacological tools for elucidating the PI3K pathway.
Bioorg Med Chem Lett
; 22(17): 5445-50, 2012 Sep 01.
Article
em En
| MEDLINE
| ID: mdl-22863202
ABSTRACT
Using a parallel synthesis approach to target a non-conserved region of the PI3K catalytic domain a pan-PI3K inhibitor 1 was elaborated to provide alpha, delta and gamma isoform selective Class I PI3K inhibitors 21, 24, 26 and 27. The compounds had good cellular activity and were selective against protein kinases and other members of the PI3K superfamily including mTOR and DNA-PK.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Tiazóis
/
Inibidores de Proteínas Quinases
/
Inibidores de Fosfoinositídeo-3 Quinase
Limite:
Animals
/
Female
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Ano de publicação:
2012
Tipo de documento:
Article