Interest of acridine derivatives in the anticancer chemotherapy

DNA is considered as one of the main targets for anticancer drug design. Th e planar structure of acridines confers to the molecules the ability to bin d DNA by intercalation and therefore to interfere with metabolic processes. A large number of natural alkaloids and synthetic acridine derivatives hav e been tested as anticancer agents. So far, a few molecules have entered cl inical trials and have been approved for chemotherapy. The mechanisms of ac tion are not fully understood. Cytotoxicity may be related to potent enzyme inhibition. Topoisomerase and telomerase activities may be strongly affect ed by acridines. The affinity of acridines for DNA has also been used to de sign new active compounds in which a DNA modifying group is tethered to the acridine nucleus. Acridine derivatives display other pharmacological prope rties such as antibacterial and antimalarial activities. They are also test ed for Alzheimer's disease.