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Synthesis and Biological Evaluation of New Quinoxaline Derivatives of ICF01012 as Melanoma-Targeting Probes

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posted on 08.05.2014 by Radhia El Aissi, Jianrong Liu, Sophie Besse, Damien Canitrot, Olivier Chavignon, Jean-Michel Chezal, Elisabeth Miot-Noirault, Emmanuel Moreau
The aim of this study was the synthesis and pharmacokinetic selection of a best melanin-targeting ligand for addressing anticancer agents to pigmented melanoma. Seven quinoxaline carboxamide derivatives were synthesized and radiolabeled with iodine-125. Biodistribution studies of compounds [125I]­1a–g performed in melanoma-bearing mice tumor showed significant tumor uptake (range 2.43–5.68%ID/g) within 1 h after i.v. injection. Fast clearance of the radioactivity from the nontarget organs mainly via the urinary system gave high tumor-to-blood and tumor-to-muscle ratios. Given its favorable clearance and high tumor-melanoma uptake at 72 h, amide 1d was the most promising melanoma-targeting ligand in this series. Compound 1d will be used as building block for the design of new melanoma-selective drug delivery systems.

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