To our knowledge, the rhizomes of Zingiber officinale (ginger) is one of the most frequently and heavily consumed spices throughout the word. Extensive studies had been undertaken to clarity the constituents of ginger and the pungent principles of ginger had been isolated and classified as zingerones, gingerols, gingerdiones, and shogaols. And it has been showed that some of ginger derivatives have anticancer activity. Furthermore, a series of zingerone derivatives, femlamides, was synthesized in our laboratory, and these compounds were assayed for their cytotoxicity against HL-60 human leukemia cells. Among them, compound DBA was the most potent against HL-60 cells with IC50 values of approximately 8.2 μM. In the present study, the anticancer mechanisms of DBA were investigated. Anticancer mechanisms were determined by using cell cycle analysis, DNA fragmentation, and RT-PCR technology. Results showed that DBA exerts its anticancer action by inducing cell cycle G2/M arrest and promoting cell apoptosis.