%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