PMID: 10649974Jan 29, 2000Paper

A potential melanoma tracer: synthesis, radiolabeling, and biodistribution in mice of a new nitridotechnetium bis(aminothiol) derivative pharmacomodulated by a N-(diethylaminoethyl)benzamide

Journal of Medicinal Chemistry
P AuzelouxJ C Madelmont

Abstract

Radioiodobenzamides are the best-known agents under study for the diagnosis of cutaneous melanoma and its metastases. We report the synthesis of a new BAT derivative radiopharmaceutical in which radioiodine is replaced by 99m-technetium. The cyclic intermediary methyl 4-[3-(4,4,7,7-tetramethyl-5,6-dithia-2, 9-diazacyclodecyl)-2-oxapropyl]benzoate (5) occurred in two different conformations identified by spectroscopic analysis. The final BAT ligand was radiolabeled using the nitridotechnetium core by a ligand-exchange reaction. Two different complexes were purified. After macroscopic 99-technetium synthesis, syn and anti isomers were identified. The global radiochemical yield was over 80%. The biodistribution of these two complexes was evaluated in mice bearing murine B16 melanoma. Extensive liver and kidney uptake was observed, but the benzamide tropism for the tumor was partially preserved.

References

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Citations

Mar 9, 2012·European Journal of Medicinal Chemistry·Carolina MouraAntónio Paulo
May 23, 2020·Proceedings of the National Academy of Sciences of the United States of America·Ayoung PyoJung-Joon Min
Mar 28, 2015·Journal of Materials Chemistry. B, Materials for Biology and Medicine·Audrey ParatDelphine Felder-Flesch
Dec 16, 2018·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Ayoung PyoJung-Joon Min
Dec 13, 2002·Journal of Medicinal Chemistry·Michael EisenhutUwe Haberkorn
Mar 16, 2006·Journal of the American Chemical Society·Amanda DonovanJohn F Valliant

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