Terpenoids (or isoprenoids) - a subclass of the prenyllipids represent the oldest and the largest group of natural compounds. Terpenoids as chemopreventive agents with reference to colon cancer and their molecular targets are reviewed. Many of the terpenoids exert its anti-colon cancer effect via cell cycle arrest and apoptosis induction. Some terpenoids are also shown to interrupt the various stages of adenoma-carcinoma sequence of colon cancer. Extensive preclinical research are warranted to achieve the bench to bedside application of terpenoids.