期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 5, 期 5, 页码 468-473出版社
AMER CHEMICAL SOC
DOI: 10.1021/ml400468x
关键词
Melanoma; melanin-targeting ligand; radiolabeling; iodine-125
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 [I-125]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 Id will be used as building block for the design of new melanoma-selective drug delivery systems.
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