Synthesis, antitumor activity, distribution and toxicity of 4-[4-[Bis(2-chloroethyl)amino]phenyl]-1-hydroxybutane-1 1-bisphosphonic acid (BAD), a new lost derivative with increased accumulation in rat osteosarcoma

@article{Wingen1986SynthesisAA,
  title={Synthesis, antitumor activity, distribution and toxicity of 4-[4-[Bis(2-chloroethyl)amino]phenyl]-1-hydroxybutane-1 1-bisphosphonic acid (BAD), a new lost derivative with increased accumulation in rat osteosarcoma},
  author={Franz Wingen and Helmut Sterz and Horst Blum and H U Moeller and W F Pittermann and Beatrice L. Pool and Hans J. Sinn and Herbert Spring and Dorothee Schmahl},
  journal={Journal of Cancer Research and Clinical Oncology},
  year={1986},
  volume={111},
  pages={209-219}
}
The aim of this study was to investigate whether the newly synthesized bisphosphonic acidlinked N-Lost derivative BAD retains bone-seeking and cytostatic properties. The paper describes experiments on mutagenicity in vitro and on toxicity in vivo. BAD is characterized by very low mutagenic activity toward histidine auxotrophic Salmonella typhimurium strains. Cytotoxic effects were tested in rat osteosarcoma and in Walker carcinosarcoma 256B. The LD50 of i.v. injected BAD was 146 mg/kg. Acute… CONTINUE READING

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