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Four Caudatin glycosides were synthesized from Caudatin by reaction with tetra-O-actyl-D-glycosyl bromide catalyzed by CdCO3 and tested in vitro for their antiproliferative activities against human lung cancer A549, human prostate cancer PC3, human liver cancer BEL-7402 and human gastric cancer SGC-7901 cells. The IC50 values indicated that the inhibitory effect of Caudatin-tetra-O-actyl-D-glycosides was superior or comparable to Caudatin against most of the tested cells, worthy of further investigation.