Synthesis and structure-activity optimization of azepane-containing derivatives as PTPN2/PTPN1 inhibitors.
Eur J Med Chem
; 270: 116390, 2024 Apr 15.
Article
in 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.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Protein Tyrosine Phosphatase, Non-Receptor Type 1
/
Protein Tyrosine Phosphatase, Non-Receptor Type 2
Language:
En
Journal:
Eur J Med Chem
Year:
2024
Document type:
Article
Affiliation country:
China
Publication country:
FR
/
FRANCE
/
FRANCIA
/
FRANÇA