Resveratrol, a well-known natural product and a major component in grape, has attracted considerable attention as one of the most promising cancer during the past decade. Many studies have established that resveratrol can exert a broad range of biological activities including ceramide-mediated proapoptotic, antineoplastic, apoptosis-inducing, etc. Most important, resveratrol has been identified as an effective candidate for cancer chemoprevention based on its striking inhibitory effects on cellular events associated with cancer initiation, promotion, and progression. This review describes the general properties of resveratrol and its potential effect against cancer including its evidences as an antitumor agent in vitro, in vivo and clinically. In addition, we also summarized the structure-activity relationship of resveratrol and its analogues regarding the antitumor effects.