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dc.contributor.authorKing, Aen_US
dc.contributor.authorDoepner, Aen_US
dc.contributor.authorTurton, Den_US
dc.contributor.authorCiobota, DMen_US
dc.contributor.authorDa Pieve, Cen_US
dc.contributor.authorWong Te Fong, A-Cen_US
dc.contributor.authorKramer-Marek, Gen_US
dc.contributor.authorChung, Y-Len_US
dc.contributor.authorSmith, Gen_US
dc.coverage.spatialEnglanden_US
dc.date.accessioned2018-03-20T14:56:48Z
dc.date.issued2018-04-25en_US
dc.identifierhttps://www.ncbi.nlm.nih.gov/pubmed/29629716en_US
dc.identifier.citationOrg Biomol Chem, 2018, 16 (16), pp. 2986 - 2996en_US
dc.identifier.urihttps://repository.icr.ac.uk/handle/internal/1603
dc.identifier.eissn1477-0539en_US
dc.identifier.doi10.1039/c8ob00432cen_US
dc.description.abstractTrifluoromethyl groups are widespread in medicinal chemistry, yet there are limited 18F-radiochemistry techniques available for the production of the complementary PET agents. Herein, we report the first radiosynthesis of the anticancer nucleoside analogue trifluridine, using a fully automated, clinically-applicable 18F-trifluoromethylation procedure. [18F]Trifluridine was obtained after two synthetic steps in <2 hours. The isolated radiochemical yield was 3% ± 0.44 (n = 5), with a radiochemical purity >99%, and a molar activity of 0.4 GBq μmol-1 ± 0.05. Biodistribution and PET-imaging data using HCT116 tumour-bearing mice showed a 2.5 %ID g-1 tumour uptake of [18F]trifluridine at 60 minutes post-injection, with bone uptake becoming a prominent feature thereafter. In vivo metabolite analysis of selected tissues revealed the presence of the original radiolabelled nucleoside analogue, together with deglycosylated and phosphorylated [18F]trifluridine as the main metabolites. Our findings suggest a potential role for [18F]trifluridine as a PET radiotracer for elucidation of drug mechanism of action.en_US
dc.format.extent2986 - 2996en_US
dc.languageengen_US
dc.language.isoengen_US
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/en_US
dc.titleRadiosynthesis of the anticancer nucleoside analogue Trifluridine using an automated 18F-trifluoromethylation procedure.en_US
dc.typeJournal Article
dcterms.dateAccepted2018-03-16en_US
rioxxterms.versionofrecord10.1039/c8ob00432cen_US
rioxxterms.licenseref.urihttps://creativecommons.org/licenses/by/4.0en_US
rioxxterms.licenseref.startdate2018-04-25en_US
rioxxterms.typeJournal Article/Reviewen_US
dc.relation.isPartOfOrg Biomol Chemen_US
pubs.issue16en_US
pubs.notesNo embargoen_US
pubs.organisational-group/ICR
pubs.organisational-group/ICR/Primary Group
pubs.organisational-group/ICR/Primary Group/ICR Divisions
pubs.organisational-group/ICR/Primary Group/ICR Divisions/Cancer Therapeutics
pubs.organisational-group/ICR/Primary Group/ICR Divisions/Cancer Therapeutics/Preclinical Molecular Imaging
pubs.organisational-group/ICR/Primary Group/ICR Divisions/Radiotherapy and Imaging
pubs.organisational-group/ICR/Primary Group/ICR Divisions/Radiotherapy and Imaging/Magnetic Resonance
pubs.organisational-group/ICR/Primary Group/ICR Divisions/Radiotherapy and Imaging/PET Radiochemistry
pubs.organisational-group/ICR/Primary Group/ICR Divisions/Radiotherapy and Imaging/Preclinical Molecular Imaging
pubs.organisational-group/ICR/Primary Group/ICR Divisions/Radiotherapy and Imaging/Radioisotope Physics
pubs.publication-statusPublisheden_US
pubs.volume16en_US
pubs.embargo.termsNo embargoen_US
icr.researchteamMagnetic Resonanceen_US
icr.researchteamPET Radiochemistryen_US
icr.researchteamPreclinical Molecular Imagingen_US
icr.researchteamRadioisotope Physicsen_US
dc.contributor.icrauthorChung, Yuen-Lien_US
dc.contributor.icrauthorDa Pieve, Chiaraen_US
dc.contributor.icrauthorKramer-Marek, Gabrielaen_US
dc.contributor.icrauthorSmith, Grahamen_US
dc.contributor.icrauthorKing, Aliceen_US


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Except where otherwise noted, this item's license is described as http://creativecommons.org/licenses/by/4.0/