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Synthesis and in Vivo Evaluation of [123I]Melanin-Targeted Agents.

Abstract：

:This study reports the synthesis, [(123)I]radiolabeling, and biological profile of a new series of iodinated compounds for potential translation to the corresponding [(131)I]radiolabeled compounds for radionuclide therapy of melanoma. Radiolabeling was achieved via standard electrophilic iododestannylation in 60-90% radiochemical yield. Preliminary SPECT imaging demonstrated high and distinct tumor uptake of all compounds, as well as high tumor-to-background ratios compared to the literature compound [(123)I]4 (ICF01012). The most favorable compounds ([(123)I]20, [(123)I]23, [(123)I]41, and [(123)I]53) were selected for further biological investigation. Biodistribution studies indicated that all four compounds bound to melanin containing tissue with low in vivo deiodination; [(123)I]20 and [(123)I]53 in particular displayed high and prolonged tumor uptake (13% ID/g at 48 h). [(123)I]53 had the most favorable overall profile of the cumulative uptake over time of radiosensitive organs. Metabolite analysis of the four radiotracers found [(123)I]41 and [(123)I]53 to be the most favorable, displaying high and prolonged amounts of intact tracer in melanin containing tissues, suggesting melanin specific binding. Results herein suggest that compound [(123)I]53 displays favorable in vivo pharmacokinetics and stability and hence is an ideal candidate to proceed with further preclinical [(131)I] therapeutic evaluation.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Roberts MP,Nguyen V,Ashford ME,Berghofer P,Wyatt NA,Krause-Heuer AM,Pham TQ,Taylor SR,Hogan L,Jiang CD,Fraser BH,Lengkeek NA,Matesic L,Gregoire MC,Denoyer D,Hicks RJ,Katsifis A,Greguric I

doi

10.1021/acs.jmedchem.5b00777

subject

Has Abstract

pub_date

2015-08-13 00:00:00

pages

6214-24

issue

15

eissn

0022-2623

issn

1520-4804

journal_volume

58

pub_type

杂志文章

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