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Synthesis of a new fluorine‐18 glycosylated ‘click’ cyanoquinoline for the imaging of epidermal growth factor receptor
Author(s) -
Pisaneschi Federica,
Slade Rozanna L.,
Iddon Lisa,
George Guillaume P. C.,
Nguyen QuangDé,
Spivey Alan C.,
Aboagye Eric O.
Publication year - 2014
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.3170
Subject(s) - chemistry , radiosynthesis , epidermal growth factor receptor , radiochemistry , yield (engineering) , tracer , click chemistry , positron emission tomography , a431 cells , azide , nuclear chemistry , receptor , cell , biochemistry , combinatorial chemistry , nuclear medicine , organic chemistry , medicine , materials science , physics , molecular medicine , cell cycle , nuclear physics , metallurgy
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.