Design, synthesis and biological evaluation of novel quinazoline derivatives as immune checkpoint inhibitors.
Bioorg Med Chem Lett
; 108: 129796, 2024 Aug 01.
Article
in En
| MEDLINE
| ID: mdl-38754563
ABSTRACT
In this work, we report 14 novel quinazoline derivatives as immune checkpoint inhibitors, IDO1 and PD-L1. The antitumor screening of synthesized compounds on ovarian cancer cells indicated that compound V-d and V-l showed the most activity with IC50 values of about 5 µM. Intriguingly, compound V-d emerges as a stand out, triggering cell death through caspase-dependent and caspase-independent manners. More importantly, V-d presents its ability to hinder tumor sphere formation and re-sensitized cisplatin-resistant A2780 cells to cisplatin treatment. These findings suggest that compound V-d emerges as a promising lead candidate for the future development of immuno anticancer agents.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Quinazolines
/
Drug Screening Assays, Antitumor
/
Drug Design
/
Immune Checkpoint Inhibitors
/
Antineoplastic Agents
Limits:
Humans
Language:
En
Journal:
Bioorg Med Chem Lett
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2024
Document type:
Article
Country of publication:
United kingdom