Synthesis of a new fluorine-18 glycosylated 'click' cyanoquinoline for the imaging of epidermal growth factor receptor.

J Labelled Comp Radiopharm

Faculty of Medicine, Comprehensive Cancer Imaging Centre, Imperial College London, Hammersmith Hospital Campus, Du Cane Road, London, W12 0NN, UK; Department of Chemistry, Imperial College London, South Kensington Campus, London, SW7 2AZ, UK.

Published: February 2014

This study reports the radiosynthesis of a new fluorine-18 glycosylated 'click' cyanoquinoline [(18) F]5 for positron emission tomography imaging of epidermal growth factor receptor (EGFR). The tracer was obtained in 47.7 ± 7.5% (n = 3) decay-corrected radiochemical yield from 2-[(18) F]fluoro-2-deoxy-β-d-glucopyranosyl azide, and the overall nondecay-corrected radiochemical yield from aqueous fluoride was 8.6 ± 2.3% (n = 3). An in vitro preliminary cellular uptake study showed selectivity of the tracer for EGFR-positive A431 cell lines versus EGFR-negative MCF-7 cell lines. [(18) F]5 tracer uptake in A431 cells was significantly reduced by addition of the cold isotope analogue compound 5.

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http://dx.doi.org/10.1002/jlcr.3170DOI Listing

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