%0 Journal Article %A Aissi, Radhia El %A Liu, Jianrong %A Besse, Sophie %A Canitrot, Damien %A Chavignon, Olivier %A Chezal, Jean-Michel %A Miot-Noirault, Elisabeth %A Moreau, Emmanuel %D 2014 %T Synthesis and Biological Evaluation of New Quinoxaline Derivatives of ICF01012 as Melanoma-Targeting Probes %U https://acs.figshare.com/articles/journal_contribution/Synthesis_and_Biological_Evaluation_of_New_Quinoxaline_Derivatives_of_ICF01012_as_Melanoma_Targeting_Probes/2298916 %R 10.1021/ml400468x.s001 %2 https://acs.figshare.com/ndownloader/files/3936481 %K Fast clearance %K ratio %K ligand %K Biological Evaluation %K Synthesi %K compound %K tumor uptake %K series %K ProbesThe %K i.v %K nontarget organs %K Compound 1 %K 72 h %K amide 1 %K Biodistribution %K synthesis %K anticancer agents %K injection %K aim %K 1 h %K iodine %K quinoxaline carboxamide derivatives %K New Quinoxaline Derivatives %K building block %K melanoma %K ID %K pharmacokinetic selection %K radiolabeled %K radioactivity %K ICF 01012 %X 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. %I ACS Publications