Potential antitumor agents. 43. Synthesis and biological activity of dibasic 9-aminoacridine-4-carboxamides, a new class of antitumor agent.

@article{Atwell1984PotentialAA,
  title={Potential antitumor agents. 43. Synthesis and biological activity of dibasic 9-aminoacridine-4-carboxamides, a new class of antitumor agent.},
  author={Graham J. Atwell and B. F. Cain and B. C. Baguley and Graeme Finlay and William A. Denny},
  journal={Journal of medicinal chemistry},
  year={1984},
  volume={27 11},
  pages={1481-5}
}
The synthesis and biological activities of representatives of a new class of antitumor agent, the N-[2-(dialkylamino)ethyl ]-9-aminoacridine-4-carboxamides, are reported. Members of this class are stable and very water soluble with high levels of in vitro and in vivo antitumor activity. The compounds bind tightly to double-stranded DNA by intercalation, but the requirements for antitumor activity are more restrictive. They depend critically on the separation distance, positioning, and pKa… CONTINUE READING

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