Benzofuran-chalcone derivatives as VEGFR-2 inhibitors: synthesis and anticancer evaluation

The discovery and development of efficient VEGFR-2 inhibitors has become a research hotspot in cancer treatment. In this work, a series of new benzofuran-based chalcone derivatives have been prepared, and in vitro anticancer activities have been evaluated. The results revealed that derivatives showed selective cytotoxic activity against HCC1806, Hela and A549 cell lines, especially 5c exhibited excellent inhibitory effect on VEFGR-2 (IC50 = 1.07 nM). The molecular docking study indicated that 5c had an obvious binding site with the target VEGFR-2 (PDB ID: 4BSK). Therefore, the benzofuran-based chalcone derivatives could be potent VEGFR-2 inhibitors.