Nitracrine and its congeners--an overview.

1. An anticancer drug, nitracrine 1-nitro-9(3'3'-dimethylaminopropylamino)acridine (Ledakrin, C-283) exhibits potent cytostatic effects which can be ascribed to interactions of the drug with DNA. 2. The reduction of the nitro group of nitracrine is one of the activation steps leading to the drug covalent binding to DNA and proteins both in subcellular systems and in the cell. 3. DNA-drug non-covalent interactions and covalent complexes are examined in several model systems and compared with the properties of a number of derivatives with programmed structural changes. 4. DNA-protein crosslinks and interstrand crosslinks are detected in the cells following exposition to the drug. 5. The drug exhibits selective toxicity and radiosensitization effects to hypoxic mammalian cells.