In recent years, a large number of new potent symmetrical cytotoxic agents that act through different mechanisms have been described. Apoptosis induction is one of the most representative of these mechanisms. Recent articles have revealed that the activation of apoptosis pathways is the key mechanism by which cytotoxic tumor cells are killed. The present review highlights the importance of the molecular symmetry of several chemical structures and their relation with cytotoxic and apoptotic activity.