Interrelations between anti-tumour activity, DNA breakage, and DNA binding kinetics for 9-aminoacridinecarboxamide anti-tumour agents.

For a series of 9-aminoacridinecarboxamides, anti-tumour activity in vivo and cytotoxicity in vitro are correlated directly with the ability of the compounds to cause DNA single-strand breaks and with their DNA-dissociation mechanisms and residence times. It is suggested that one important consequence of long DNA residence times may be an enhanced ability to cause DNA strand breaks by a non-oxidative mechanism.