Technical Abstract: Colon cancer is one of the leading causes of cancer death in men and women in Western countries. Epidemiological studies have linked consumption of fruits and vegetables to a reduced risk of colon cancer, and small fruits are particularly rich sources of many active phytochemical stilbenes, such as resveratrol and pterostilbene. Recent advances in prevention of colon cancer have stimulated an interest in diet and lifestyle as an effective means of intervention in development of the disease. As constituents of grapes, red wine and small fruits, stilbenes are under intense investigation as cancer chemopreventive agents. Stilbenes have diverse pharmacological activities, which include cancer chemoprevention, cholesterol-lowering, enhanced insulin sensitivity, and increased lifespan. One of the best-characterized stilbenes, resveratrol, has been known as an antioxidant, and anti-aging as well as anti-inflammatory agent. This review summarizes results related to a potential use of various stilbenes as cancer chemopreventive agents, mainly in vitro mechanisms of action, pharmacokinetics, and efficacy in prevention of colon cancer in animals and humans.