Sixteen thiosemicarbazones 2～4 were synthesized from following three steps: firstly hydrazine reacted with carbon disulfide and dimethyl sulfate to form methyl hydrazino-dithiocarboxylate with yield of 60%, which further reacted with ketone or aldehyde in i-PrOH to give 1a～1h with yields of 78%～96%. Treatment of compound 1 with piperazine, N-substituted piperazine or morpholine in ethanol afforded 2～4 in 57%～84% yields. All compounds were characterized by elemental analysis, MS, IR and ¹H NMR spectra. The antibacterial and anticancer activities in vitro of all compounds have been determined. The results show that compound 3f possess strong antibacterial activity while the compound 4c possess anticancer activity.

Key words: synthesis, anticancer, antibacterial activity, thiosemicarbozones