1.
Bioorg Med Chem Lett
; 22(17): 5445-50, 2012 Sep 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-22863202
RESUMO
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.
Assuntos
Inibidores de Fosfoinositídeo-3 Quinase , Inibidores de Proteínas Quinases/química , Inibidores de Proteínas Quinases/farmacologia , Tiazóis/química , Tiazóis/farmacologia , Animais , Domínio Catalítico , Feminino , Humanos , Camundongos , Modelos Moleculares , Fosfatidilinositol 3-Quinases/química , Fosfatidilinositol 3-Quinases/metabolismo , Isoformas de Proteínas/antagonistas & inibidores , Isoformas de Proteínas/química , Isoformas de Proteínas/metabolismo , Inibidores de Proteínas Quinases/farmacocinética , Ratos , Transdução de Sinais/efeitos dos fármacos , Tiazóis/farmacocinética
2.
Bioorg Med Chem
; 12(19): 5213-24, 2004 Oct 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-15351404
RESUMO
A series of novel corticosteroid derivatives featuring C-17 furoate ester functionality have been synthesised. Profiling in vitro and in vivo has resulted in the identification of a compound with a longer duration of action and a lower oral side effect profile in rodents compared to budesonide.
