Abstract: | In order to elucidate the mechanism of deoxyribonucleic acid (DNA) strand breaks caused by 9-anilino-acridine DNA intercalators, the antitumor activity of L1210, P388 and the reduction-oxidation (redox) reaction of 9-anilinoacridines were studied. The redox reaction induced by two electrons causing structural changes in quinone diimines of 9-anilinoacridines is believed to be an important factor in DNA strand breaks and was examined by means of temperature-dependent nuclear magnetic resonance and cyclic voltammetry. The redox reaction of 9-anilinoacridines is induced by the effect of a low-energy electron transfer from the acridine to the aniline ring. We propose that the redox reaction plays an important role in the DNA strand cleavage of 9-anilinoacridine when it is intercalated into double-strand DNA. |