Benzofuran-Chalcone Derivatives as VEGFR-2 Inhibitors: Synthesis and Anticancer Evaluation

Area of Science:

• Medicinal Chemistry
• Oncology
• Molecular Biology

Background:

• Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2) is a critical target in cancer therapy.
• Developing selective and potent VEGFR-2 inhibitors is a significant research area.
• Chalcone derivatives are explored for their diverse biological activities.

Purpose of the Study:

• To synthesize and evaluate novel benzofuran-based chalcone derivatives as potential anticancer agents.
• To investigate the inhibitory activity of these compounds against VEGFR-2.
• To explore the binding interactions of the most potent compound with VEGFR-2.

Main Methods:

• Chemical synthesis of benzofuran-based chalcone derivatives.
• In vitro cytotoxic activity evaluation against various cancer cell lines (HCC1806, Hela, A549).
• Enzyme inhibition assays to determine VEGFR-2 inhibitory potency (IC50).
• Molecular docking studies to predict binding interactions with VEGFR-2 (PDB ID: 3V6B).

Main Results:

• The synthesized derivatives exhibited selective cytotoxic effects on tested cancer cell lines.
• Compound 5c demonstrated potent inhibition of VEGFR-2 with an IC50 value of 1.07 nM.
• Molecular docking confirmed a favorable binding interaction of compound 5c within the VEGFR-2 active site.

Conclusions:

• Benzofuran-based chalcone derivatives represent a promising class of compounds for cancer treatment.
• Compound 5c is a potent inhibitor of VEGFR-2 and warrants further investigation.
• These findings support the development of novel VEGFR-2 inhibitors based on this scaffold.