AI Article Synopsis
- Researchers have developed 14 new quinazoline derivatives that act as immune checkpoint inhibitors targeting IDO1 and PD-L1.
- Two compounds, V-d and V-l, showed significant anti-tumor activity against ovarian cancer cells with low IC values.
- Compound V-d is particularly notable for promoting cell death in different ways and for reversing cisplatin resistance in specific ovarian cancer cells, suggesting its potential as a new cancer treatment.
Article 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 IC 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.
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| http://dx.doi.org/10.1016/j.bmcl.2024.129796 | DOI Listing |
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