Doxoform and Daunoform: anthracycline-formaldehyde conjugates toxic to resistant tumor cells.

@article{Fenick1997DoxoformAD,
  title={Doxoform and Daunoform: anthracycline-formaldehyde conjugates toxic to resistant tumor cells.},
  author={David J. Fenick and Dylan J. Taatjes and Tad H. Koch},
  journal={Journal of medicinal chemistry},
  year={1997},
  volume={40 16},
  pages={2452-61}
}
The recent discovery that the clinically important antitumor drugs doxorubicin and daunorubicin alkylate DNA via catalytic production of formaldehyde prompted the synthesis of derivatives bearing formaldehyde. Reaction of the parent drugs with aqueous formaldehyde at pH 6 produced in 40-50% yield conjugates consisting of two molecules of the parent drug as oxazolidine derivatives bound together at their 3'-nitrogens by a methylene group. The structures were established as bis(3'-N-(3'-N,4'-O… CONTINUE READING
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