Evaluation of radiolabeled (hetero)aromatic analogues of N-(2-diethylaminoethyl)-4-iodobenzamide for imaging and targeted radionuclide therapy of melanoma.

Abstract	Targeted radionuclide therapy using radioiodinated compounds with a specific affinity for melanoma tissue is a promising treatment for disseminated melanoma, but the candidate with the ideal kinetic profile remains to be discovered. Targeted radionuclide therapy concentrates the effects on tumor cells, thereby increasing the efficacy and decreasing the morbidity of radiotherapy. In this context, analogues of N-(2-diethylaminoethyl)-4-iodobenzamide (BZA) are of interest. Various (hetero)aromatic analogues 5 of BZA were synthesized and radioiodinated with (125)I, and their biodistribution in melanoma-bearing mice was studied after i.v. administration. Most [ (125)I] 5-labeled compounds appeared to bind specifically and with moderate-to-high affinity to melanoma tumor. Two compounds, 5h and 5k, stood out with high specific and long-lasting uptake in the tumor, with a 7- and 16-fold higher value than BZA at 72 h, respectively, and kinetic profiles that makes them promising agents for internal targeted radionuclide therapy of melanoma.
Authors	Jean-Michel Chezal, Janine Papon, Pierre Labarre, Claire Lartigue, Marie-Josephe Galmier, Caroline Decombat, Olivier Chavignon, Jean Maublant, Jean-Claude Teulade, Jean-Claude Madelmont, Nicole Moins
Journal	Journal of medicinal chemistry (J Med Chem) Vol. 51 Issue 11 Pg. 3133-44 (Jun 12 2008) ISSN: 0022-2623 [Print] United States
PMID	18481842 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References	Benzamides Iodine Radioisotopes Melanins N-(2-diethylaminoethyl)-6-iodoquinoline-2-carboxamide N-(2-diethylaminoethyl)-6-iodoquinoxaline-2-carboxamide Quinolines Quinoxalines Radiopharmaceuticals
Topics	Animals Benzamides (chemical synthesis, chemistry, pharmacokinetics) Iodine Radioisotopes Male Melanins (chemistry) Melanoma, Experimental (diagnostic imaging, metabolism, therapy) Mice Mice, Inbred C57BL Quinolines (chemical synthesis, chemistry, pharmacokinetics) Quinoxalines (chemical synthesis, chemistry, pharmacokinetics) Radionuclide Imaging Radiopharmaceuticals (chemical synthesis, chemistry, pharmacokinetics) Structure-Activity Relationship Tissue Distribution

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