Design,Synthesis and Anticancer Activity Evaluation of HDAC6 Inhibitors Containing Chalcone Fragments
Chalcone has various biological activities such as anti-cancer,anti-inflammatory,and antioxidant.Histone deacetylase 6(HDAC6)is an important anti-cancer target.According to the principle of molecular hybridization,5 HDAC6 inhibitors containing chalcone fragment were designed and synthesized,and evaluated anticancer activity against gastric cancer cells and inhibition of HDAC6 protein in vitro.The results showed that the target compounds had strong inhibition against gastric cancer cells HGC27 and MGC803,with IC50 values ranging from 1.0 to 7.4 pM.They also exhibited strong inhibition against HDAC6 protein in vitro,with an IC50 value ranging from 4.6 to 47.8 nM.Among them,compound 17 had the strongest cytotoxicity against gastric cancer cells HGC27 and MGC803,and also exhibited the strongest affinity with HDAC6 protein.Molecular docking also confirmed the results.These results indicate that HDAC6 inhibitors containing chalcone structures are worth further investigation.
万方数据
维普
