A series of 4 (3H)-quinazolinone derivatives with dithiocarbamate side chains were synthesized and tested for their in vitro antitumor activity against human myelogenous leukemia K562 cells. Among them,(3, 4-dihydro-2-methyl-4-oxoquinazolin-6-yl) methyl 4-(4- fluorophenyl) piperazine-1-carbodithioate 8q exhibited significant inhibitory activity against K562 cells with IC50 value of 0.5 μM.