Discovery of Highly Isoform Selective Thiazolopiperidine Inhibitors of Phosphoinositide 3-Kinase γ.
J Med Chem
; 58(14): 5684-8, 2015 Jul 23.
Article
em En
| MEDLINE
| ID: mdl-26121481
ABSTRACT
A series of high affinity second-generation thiazolopiperidine inhibitors of PI3Kγ were designed based on some general observations around lipid kinase structure. Optimization of the alkylimidazole group led to inhibitors with higher levels of PI3Kγ selectivity. Additional insights into PI3K isoform selectivity related to sequence differences in a known distal hydrophobic pocket are also described.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Piperidinas
/
Inibidores Enzimáticos
/
Descoberta de Drogas
/
Inibidores de Fosfoinositídeo-3 Quinase
Limite:
Humans
Idioma:
En
Revista:
J Med Chem
Assunto da revista:
QUIMICA
Ano de publicação:
2015
Tipo de documento:
Article
País de afiliação:
Estados Unidos