Resveratrol has been identified as a potent anticancer agent in a variety of studies. In this study, several resveratrol derivatives were synthesized and investigated in the search for an anticancer agent with higher efficacy than resveratrol. During our examination of cancer cell lines, compounds C, F, and G evidenced higher inhibitory activity than resveratrol with regard to the growth of PC-3 and LNCaP human prostate cancer cells. Moreover, four derivatives of resveratrol evidenced potent growth inhibitory activity (IC50 0.01-0.04 microM) in LNCaP cells. The levels of activity in these derivatives were 25-100 times stronger than that associated with resveratrol (IC50 1.0 microM). Our results suggested that compounds C, D, F, and G might function as anticancer agents on prostate tumors. This study also contains a discussion regarding the structure-activity relationships of several resveratrol derivatives.