Abstract: Novel synthetic bis(benzylidene-benzenamine)disulfides and the preparation method are disclosed in the present invention. These compounds are afforded with the oxidizing reagent at low temperature and short time period via intra-molecular coupling reaction. In vitro experiments have been revealed that bis-disulfides are cytotoxic to cancer cells, especially human breast cancer cells MCF-7. Additionally, bis-disulfides arrest the cell cycle at sub-G1 phase and increase p38 phosphorylation to result in apoptosis. Bis-disulfides also inhibit growth of murine melanoma B16 cells but have no cytotoxicity to human fibroblasts. Bis-disulfides also can reduce murine melanoma size in the mouse model. The prepared compounds of the invention would be applicable in anticancer and anti-tumor therapies.

Abstract: Novel synthetic bis(benzylidene-benzenamine)disulfides and the preparation method are disclosed in the present invention. These compounds are afforded with the oxidizing reagent at low temperature and short time period via intra-molecular coupling reaction. In vitro experiments have been revealed that bis-disulfides are cytotoxic to cancer cells, especially human breast cancer cells MCF-7. Additionally, bis-disulfides arrest the cell cycle at sub-G1 phase and increase p38 phosphorylation to result in apoptosis. Bis-disulfides also inhibit growth of murine melanoma B16 cells but have no cytotoxicity to human fibroblasts. Bis-disulfides also can reduce murine melanoma size in the mouse model. The prepared compounds of the invention would be applicable in anti-cancer and anti-tumor therapies.