Acridine/Acridone Derivatives as Catalytic Inhibitors of Topoisomerase I

Derivatives of acridine and acridone are known to intercalate into DNA and inhibit the function of topoisomerases (Topo), particularly Topo I and Topo II. These compounds usually block the ability of Topos to alter DNA supercoiling, a key process required for proper DNA replication, transcription, and repair. This study provides a literature review of more than a hundred acridine or acridone derivatives, which are known to act as Topo I inhibitors, and also presents the results of our own project in this field. The review examines the applicability of these derivatives and explores new perspectives for their development as future anticancer therapies.