Design, synthesis, and biological evaluation of new mitonafide derivatives as potential antitumor drugs

A series of potential DNA-binding antitumor agents, 2-[ω-(alkylamino)alkyl]-6-{[ω-(alkylamino)alkyl]amino}-1H-benzo[de]isoquinolin-1,3(2H)-diones and 1,7-bis{6-[(ω-(dimethylamino)alkyl)amino]-1,3-dioxo-1H-benzo[de]isoquinolin-2(3H)-yl}-4-methyl-4-azaheptanes, have been prepared as mitonafide derivatives. Their DNA-binding ability and cytotoxic activity have been evaluated. Some of the target compounds have shown high DNA affinity as well as relevant cytotoxic properties.

2-[2-(Dimethylamino)ethyl]-6-{[2-(dimethylamino)ethyl]amino}-5-nitro-1H-benzo[de]isoquinolin-1,3(2H)-dione and 1,7-bis{6-[(2-(dimethylamino)ethyl)amino]-1,3-dioxo-1H-benzo[de]isoquinolin-2(3H)-yl}-4-methyl-4-azaheptaneFigure optionsDownload as PowerPoint slide