Abstract
DNA remains one of the main targets in antitumour drug design. Due to their polycyclic planar structure, acridines interact with DNA by intercalation between base pairs and interference with essential metabolic processes. A large number of natural and synthetic acridines have been tested as anticancer agents and, so far, a few molecules have entered clinical trials and have been approved for chemotherapy. The mechanisms of action are not fully understood, however, interference with the activity of critical enzymes such as topoisomerases and telomerases has been evidenced. Other cellular targets have been identified, such as cyclin-dependent kinases and multi-drug resistance processes.