Mitochondria have emerged recently as a novel, intriguing target for anti-caner drugs, owing largely to their importance for proper growth of cancer cells. Destabilization of mitochondria often results in the induction of apoptosis in cancer cells that, consequently, may translate into suppression of tumour growth. A class of mitochondria-targeting compounds, mitocans, comprises several groups of agents with different targets within the mitochondrion. Of these, vitamin E analogues have been recently promoted as agents that disrupt mitochondria by several modes of action. These compounds hold substantial promise as potential anti-cancer drugs of clinical relevance.