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Radioactive 7-Iodo-6-Deoxytetracycline in Tumour Tissue

Abstract

THE observation1,2 that several of the tetracyclines are localized in various tumour tissues for prolonged periods of time suggested the possible utility of a tetracycline labelled with iodine-131 in the detection of neoplastic disease by the use of external body-scanning techniques. In a recent communication3 from this Laboratory, the preparation of 7-iodo-6-deoxytetracycline was described; this was the first report of an iodotetracycline of unequivocal chemical structure. A labelled iodo (131) derivative was prepared by essentially the same method, by the reaction of N-iodosuccinimide4 (131I) and 6-deoxy-tetracycline in concentrated sulphuric acid:

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References

  1. Rall, D. P., Loo, T. L., Lane, M., and Kelley, M. G., J. Nat. Cancer Inst., 19, 79 (1957).

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  2. Loo, T. L., Titus, E. D., and Rall, D. P., Science, 126, 253 (1957).

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  3. Boothe, J., Hlavka, J., Petisi, J., and Spencer, J., J. Amer. Chem. Soc., 82, 1253 (1960).

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  4. The N-iodosuccinimide (131I) was prepared by a modification of the method of Djerassi, C., J. Amer. Chem. Soc., 75, 3494 (1953), using radioiodine and N-silversuccinimide.

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  5. Kelly, R., and Buyske, D. A., J. Pharm. and Exp. Therap. (in the press).

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HLAVKA, J., BUYSKE, D. Radioactive 7-Iodo-6-Deoxytetracycline in Tumour Tissue. Nature 186, 1064–1065 (1960). https://doi.org/10.1038/1861064b0

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