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Antitumour Activity of N-(β,β′-dichlorodiethylaminomethyl)-tetra-cycline, ‘Tetracycline-mustard’

Abstract

LOCALIZATION of tetracycline in tumour tissue has been reported with both human and animal neoplasms1. Though the tetracycline class antibiotics have no antitumour effect by themselves, the possibility of using them as carriers of more potent agents seemed worthy of investigation. As a model system a nitrogen mustard (HN2) derivative was considered most practical because of simplicity of structure, availability of starting materials and general knowledge concerning the antitumour activity of mustard type alkylating agents.

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References

  1. Rall, D. P., Loo, T. L., Lane, M., and Kelly, M. G., J. Nat. Cancer Inst., 19, 79 (1957). McLeay, J. F., Amer. J. Surg., 96, 415 (1958). Dunn, A. L., Eskelson, C. D., McLeay, J. F., Ogborn, R. E., and Walske, B. R., Proc. Soc. Exp. Biol. and Med., 104, 12 (1960). Klinger, J., and Katz, R., Gastroenterol., 41, 29 (1961). Milch, R. A., Tobie, J. E., and Robinson, R. A., J. Histochem. and Cytochem., 9, 261 (1961).

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KAPLAN, M., BRADNER, W., BUCKWALTER, F. et al. Antitumour Activity of N-(β,β′-dichlorodiethylaminomethyl)-tetra-cycline, ‘Tetracycline-mustard’. Nature 205, 399–400 (1965). https://doi.org/10.1038/205399a0

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