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

Cancer is one of the most significant public health problems worldwide, and the discovery and development of efficient VEGFR-2 inhibitors has been a research hotspot in cancer treatment. In the present work, a series of novel benzofuran-based chalcone derivatives have been prepared, and in vitro anti-tumor activities of them have been evaluated. The results indicated that the compounds displayed potent anticancer activity against HCC1806, HeLa and A549 cell lines. The preliminary mechanism study showed that 4g could effectively induce the apoptosis of HCC1806 cells, and showed inhibitory effect on VEFGR-2. The molecular docking study indicated that 4g had an obvious binding site with the target VEGFR-2 (PDB ID: 4BSK). Therefore, the benzofuran-based chalcone derivatives could be considered as potent VEGFR-2 inhibitors.