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Synthesis and Biological Evaluation of New Quinoxaline Derivatives of ICF01012 as Melanoma-Targeting Probes
journal contribution
posted on 2014-05-08, 00:00 authored by Radhia El Aissi, Jianrong Liu, Sophie Besse, Damien Canitrot, Olivier Chavignon, Jean-Michel Chezal, Elisabeth Miot-Noirault, Emmanuel MoreauThe
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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Fast clearanceratioligandBiological EvaluationSynthesicompoundtumor uptakeseriesProbesThei.vnontarget organsCompound 172 hamide 1Biodistributionsynthesisanticancer agentsinjectionaim1 hiodinequinoxaline carboxamide derivativesNew Quinoxaline Derivativesbuilding blockmelanomaIDpharmacokinetic selectionradiolabeledradioactivityICF 01012
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