Discovery of 4-Azaindole Inhibitors of TGFßRI as Immuno-oncology Agents.
ACS Med Chem Lett
; 9(11): 1117-1122, 2018 Nov 08.
Article
em En
| MEDLINE
| ID: mdl-30429955
ABSTRACT
The multifunctional cytokine TGFß plays a central role in regulating antitumor immunity. It has been postulated that inhibition of TGFß signaling in concert with checkpoint blockade will provide improved and durable immune response against tumors. Herein, we describe a novel series of 4-azaindole TGFß receptor kinase inhibitors with excellent selectivity for TGFß receptor 1 kinase. The combination of compound 3f and an antimouse-PD-1 antibody demonstrated significantly improved antitumor efficacy compared to either treatment alone in a murine tumor model.
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1
Coleções:
01-internacional
Base de dados:
MEDLINE
Idioma:
En
Revista:
ACS Med Chem Lett
Ano de publicação:
2018
Tipo de documento:
Article
País de afiliação:
Estados Unidos