Synthetic cinnamylphenol derivatives as cancer chemopreventive agents

Several substituted cinnamylphenol (1,3-diphenylpropene) derivatives were synthesized and tested for their inhibitory activities against in vitro Epstein-Barr virus early antigen activation induced by 12-O-tetradecanoylphorbol-13-acetate in Raji cells. The prenylated cinnamylphenols were found to show remarkably potent activity. Furthermore, prenylated cinnamylphenols (19 and 25) exhibited a marked inhibitory effect on mouse skin tumor promotion in an in vivo two-stage carcinogenesis test. These results indicate that some prenylated cinnamylphenols might be valuable as potential cancer chemopreventive agents (anti-tumor promoters).

Graphical abstractSeveral substituted cinnamylphenol (1,3-diphenylpropene) derivatives showed anti-tumor-promoting activity on Epstein-Barr virus early antigen activation induced by TPA in Raji cells. Furthermore, prenylated cinnamylphenols (19 and 25) exhibited a marked inhibitory effect on mouse skin tumor promotion in an in vivo two-stage carcinogenesis test.Figure optionsDownload full-size imageDownload as PowerPoint slide