Synthesis and properties of bis(2,2-dimethylaziridinyl)phosphinic amides: a series of new antineoplastic agents.

@article{Macdiarmid1985SynthesisAP,
  title={Synthesis and properties of bis(2,2-dimethylaziridinyl)phosphinic amides: a series of new antineoplastic agents.},
  author={J. Macdiarmid and W. Rose and W. Biddle and M. Perlman and R. Breiner and J. Ambrus and T. Bardos},
  journal={Journal of medicinal chemistry},
  year={1985},
  volume={28 11},
  pages={
          1685-91
        }
}
In continuation of efforts to improve the antitumor selectivity of the 2,2-dimethylaziridine class of alkylating agents, a series of N-substituted bis(2,2-dimethyl-1-aziridinyl)phosphinic amides has been synthesized and evaluated. All of these compounds (3-15) were tested in vivo against leukemia P-388 in mice, where most of them caused significant increase of survival time at nontoxic dose levels. Some of the most active compounds were also tested against leukemia L1210, B16 melanoma, and… Expand
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