Abstract:

To identify new molecular agents targeted liver cancer， 12 cinnamamide compounds L10－L21 are designed and synthesized using YSM-13 as the initial compound. The structures of target compounds L10－L21 are characterized by hydrogen nuclear magnetic resonance spectroscopy， carbon spectroscopy and mass spectrometry. The inhibitory effect of the target compounds on the activity of HepG2 cells is further evaluated by cytotoxicity， cell proliferation and clone formation experiments. As the results of cytotoxicity experiments shown， （S）-cinnamamide compounds exhibit better anti-cancer activity than （R）-cinnamamide compounds， and the target compounds without an exocyclic double bond has almost no anti-cancer activity. In addition， halogen atoms F， Cl， Br para-substituted benzene ring or difluoro meta-substituted benzene ring can significantly improve the anti-liver cancer activity of the target compounds. Among them， the target compound （S，E）-3-（4-Chlorophenyl）-N-（1，2，3，4-tetrahydronaphthalen-1-yl）acrylamide （L16） perform best in anti-cancer activity， and the survival rate of HepG2 cells in the L16-administered group is only 26.36% of that in the control groups. The results of cell proliferation and clone formation experiments show that L16 could significantly inhibit the malignant proliferation ability of liver cancer cells in vitro. In summary， further study on compound L16 as a potential anti-HCC small molecule drug， and the biological mechanism of its anti-HCC activity is needed.

Key words: Cinnamamide compounds, Liver cancer, Structure-activity relationships