【文章名】Evaluation of Radiolabeled (Hetero)Aromatic Analogues of N-(2-diethylaminoethyl)-4-iodobenzamide for Imaging and Targeted Radionuclide Therapy of Melanoma.
Evaluation of Radiolabeled (Hetero)Aromatic Analogues of N-(2-diethylaminoethyl)-4-iodobenzamide for Imaging and Targeted Radionuclide Therapy of Melanoma.
[摘要]：Targeted radionuclide therapy using radioiodinated compds. 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 concs. the effects on tumor cells, thereby increasing the efficacy and decreasing the morbidity of radiotherapy. In this context, analogs of N-(2-diethylaminoethyl)-4-iodobenzamide (BZA) are of interest. Various (hetero)arom. analogs 5 of BZA were synthesized and radioiodinated with 125I, and their biodistribution in melanoma-bearing mice was studied after i.v. administration. Most [125I]5-labeled compds. appeared to bind specifically and with moderate-to-high affinity to melanoma tumor. Two compds., 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, resp., and kinetic profiles that makes them promising agents for internal targeted radionuclide therapy of melanoma.
