Synthesis and structure-activity optimization of azepane-containing derivatives as PTPN2/PTPN1 inhibitors.
Eur J Med Chem
; 270: 116390, 2024 Apr 15.
Article
em En
| MEDLINE
| ID: mdl-38604096
ABSTRACT
Protein tyrosine phosphatases PTPN2 and PTPN1 (also known as PTP1B) have been implicated in a number of intracellular signaling pathways of immune cells. The inhibition of PTPN2 and PTPN1 has emerged as an attractive approach to sensitize T cell anti-tumor immunity. Two small molecule inhibitors have been entered the clinic. Here we report the design and development of compound 4, a novel small molecule PTPN2/N1 inhibitor demonstrating nanomolar inhibitory potency, good in vivo oral bioavailability, and robust in vivo antitumor efficacy.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Proteína Tirosina Fosfatase não Receptora Tipo 1
/
Proteína Tirosina Fosfatase não Receptora Tipo 2
Idioma:
En
Ano de publicação:
2024
Tipo de documento:
Article