Alpha-tocopherol is a very well-known potent antioxidant and radical scavenger in chemical and biological systems. Its structure has served as starting point for design and synthesis of more potent antioxidant analogues with regard to its potential clinical and nutritional applications in human health. Furthermore, in recent years, intense research has been made not only in the development of hybrid compounds with classical drug moieties in a single molecule, but also in the preparation of label analogues with application in tocopherol metabolism studies. In the present review principal progresses in these aspects are outlined.