Synthesis and anti-tumor activity of new benzofuran-based chalcone derivatives as potent VEGFR-2 inhibitors

Area of Science:

• Medicinal Chemistry
• Oncology
• Molecular Biology

Background:

• Cancer remains a major global health challenge, driving the search for effective treatments.
• Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2) inhibitors are a key focus in cancer therapy research.

Purpose of the Study:

• To synthesize and evaluate novel benzofuran-based chalcone derivatives for anticancer properties.
• To investigate the mechanism of action and target interaction of promising compounds.

Main Methods:

• Synthesis of a series of novel benzofuran-based chalcone derivatives.
• In vitro evaluation of anti-tumor activity against HCC1806, HeLa, and A549 cancer cell lines.
• Preliminary mechanism studies including apoptosis induction and VEGFR-2 inhibition assays, alongside molecular docking.

Main Results:

• The synthesized compounds demonstrated potent anticancer activity across tested cell lines.
• Compound 4g effectively induced apoptosis in HCC1806 cells.
• Compound 4g exhibited inhibitory effects on VEGFR-2, with molecular docking confirming a strong binding site (PDB ID: 4BSK).

Conclusions:

• Benzofuran-based chalcone derivatives show significant promise as anticancer agents.
• These compounds, particularly 4g, act as effective VEGFR-2 inhibitors.
• Further development of these derivatives could lead to novel cancer therapeutics.