Potent inhibitors of phosphatidylinositol 3 (PI3) kinase that have antiproliferative activity only when delivered as prodrug forms.
ChemMedChem
; 8(6): 914-8, 2013 Jun.
Article
em En
| MEDLINE
| ID: mdl-23568455
ABSTRACT
Prodrugs for PI3K A series of substituted analogues of the phosphatidylinositol 3 kinase (PI3K) inhibitor LY294002 were prepared and found to potently inhibit the isolated enzyme but not MCF7 cell proliferation. Two tetrazolyl-substituted analogues were further derivatized as prodrugs resulting in restoration of cell-based activity. These data provide a conceptual model for development of tumor-targeting prodrug forms of cell-impermeable PI3K inhibitors.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Pró-Fármacos
/
Morfolinas
/
Cromonas
/
Inibidores de Proteínas Quinases
/
Inibidores de Fosfoinositídeo-3 Quinase
/
Antineoplásicos
Idioma:
En
Ano de publicação:
2013
Tipo de documento:
Article
País de afiliação:
Austrália