The potential cancer-preventive effects of resveratrol, evident from the data obtained by various studies, are summarized in this review. Resveratrol (trans-3,5,4′-trihydroxystilbene), a naturally occurring polyphenolic compound, was first isolated in 1940 as a constituent of the roots of white Hellebore (Veratrum grandiflorum O. Loes), and is now found to be present in various plants including grapes, berries, peanuts, and red wine. This review first briefly describes the current evidence on the link between resveratrol and cancer occurrence, based on epidemiological studies. Subsequently, investigations with resveratrol in animal models of colon carcinogenesis are presented, followed by a comprehensive compilation of resveratrol on cancer. In the second part, the article focuses on results from investigations on cancer-preventive mechanisms of resveratrol. Biological activities including antioxidant effects, modulation of carcinogen metabolism, anti-inflammatory potential, antioxidant properties, antiproliferative mechanisms by induction of apoptosis, and cell differentiation are discussed. Some novel information on its modulating effects on cell signaling pathway, metabolism studies, bioavailability, and cancer-preventive efficacy is also provided. Based on these findings, resveratrol may be used as a promising candidate for cancer chemoprevention.