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Acridines have been used as chemotherapeutic agents against bacteria, protozoa and fungi, and they now find important use as anticancer drugs. There is a paucity of crystal structures of acridine-DNA complexes above the dinucleotide level, but recent structures of acridinecarboxamide topoisomerase II poisons complexed to hexanucleotides have allowed a molecular rationalization of their structure-activity relationships for cytotoxicity and for their kinetics of DNA binding.