No abstract

A series of flavonoid derivatives bearing trimethoxyphenyl and benzimidazole were designed, synthesized and evaluated as potential anti-tumor agents. Compound 5g showed remarkable inhibitory activity against SGC-7901, HGC-27 and MCF-7 (IC50 values of 20.5±5.93, 3.3±2.53 and 16.6±0.75 μM, respectively), and had great selectivity to cancer cells. The results of Hoechst 33258 staining and Annexin V-FITC/PI dual staining confirmed that compound 5g induced apoptosis of the HGC-27 cells in a concentration-dependent manner. After treatment with compound 5g, the expression of HIF-1α, VEGF and PKM2 were down-regulated, accompanied by weakened the levels of lactate. Further research revealed that compound 5g could obviously inhibit tubulin assembly. In summary, compound 5g possessed a promising potential for further development into anti-tumor drug candidates.