Discovery of a Potential Multi-Target Anti-Tumor Agent via Structural Modification on Flavonoid

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