Add time:07/22/2019         Source:sciencedirect.com

Interest in the development of radiopharmaceuticals suitable for the diagnosis and treatment of malignant melanoma prompted the present study. One of the first approaches to this problem has involved the synthesis of suitably labeled precursors of melanin with the hope that these substances would be selectively taken up by the pigmented tumor and rapidly converted to a radiolabeled melanin within the tumor. Since 5, 6-dihydroxyindole is a late precursor of melanin, the synthesis of this material labeled with 14C was undertaken. This substance, however, proved to be too unstable and was therefore converted to the diacetate for animal studies. The radio-iodine-labeled analog was prepared by iodine exchange of 5,6-diacetoxy-7-iodoindole with sodium iodide-125I. Neither 5,6-diacetoxyindole-2-14C nor the 125I analog showed a predilection for melanomas in mice.

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