Zhang Chunfei, Liu Yixin, Zhang Xiao, Wan Chunping, Mao Zewei
School of Chinese Materia Medica, School of Clinical Medicine, Yunnan University of Chinese Medicine Kunming 650500 PR China
Chuxiong Autonomous Prefecture Hospital of Traditional Chinese Medicine Chuxiong 675000 PR China.
RSC Med Chem. 2024 Oct 16;16(1):392-9. doi: 10.1039/d4md00621f.
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 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.
癌症是全球最重要的公共卫生问题之一，高效VEGFR-2抑制剂的发现与开发一直是癌症治疗领域的研究热点。在本研究中，制备了一系列新型的基于苯并呋喃的查尔酮衍生物，并对它们的抗肿瘤活性进行了评估。结果表明，这些化合物对HCC1806、HeLa和A549细胞系显示出强大的抗癌活性。初步机制研究表明，4g能有效诱导HCC1806细胞凋亡，并对VEFGR-2有抑制作用。分子对接研究表明，4g与靶标VEGFR-2（PDB编号：4BSK）有明显的结合位点。因此，基于苯并呋喃的查尔酮衍生物可被视为有效的VEGFR-2抑制剂。
