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
Rall, D. P., Loo, T. L., Lane, M., and Kelley, M. G., J. Nat. Cancer Inst., 19, 79 (1957).
Loo, T. L., Titus, E. D., and Rall, D. P., Science, 126, 253 (1957).
Boothe, J., Hlavka, J., Petisi, J., and Spencer, J., J. Amer. Chem. Soc., 82, 1253 (1960).
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.
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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DOI: https://doi.org/10.1038/1861064b0
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