Design, synthesis and biological evaluation of novel quinazoline derivatives as immune checkpoint inhibitors

We are happy to announce that Dr. Ngo Son Tung and colleagues recently published their work entitled “Design, synthesis and biological evaluation of novel quinazoline derivatives as immune checkpoint inhibitors" in the Bioorganic & Medicinal Chemistry Letters.

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.