Synthesis and anticancer activities of 6-amino amonafide derivatives

@article{Norton2008SynthesisAA,
  title={Synthesis and anticancer activities of 6-amino amonafide derivatives},
  author={John Thomas Norton and Mark A. Witschi and Lynn Luong and Akane Kawamura and Supurna Ghosh and M. Sharon Stack and Edith Sim and Michael J. Avram and Daniel H. Appella and Sui Huang},
  journal={Anti-Cancer Drugs},
  year={2008},
  volume={19},
  pages={23-36}
}
Amonafide is a DNA intercalator and topoisomerase II inhibitor in clinical development for the treatment of neoplastic diseases. Amonafide contains a free arylamine, which causes it to be metabolized in humans by N-acetyl transferase-2 (NAT2) into a toxic form. To eliminate the NAT2 acetylation of amonafide while retaining the anticancer properties, we have synthesized nine derivatives that are structurally similar to amonafide that should not be acetylated. Eight derivatives have arylamines at… 
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