Radiolabeling and in vitro evaluation of a new 5-fluorouracil derivative with cell culture studies

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dc.contributor.authorIlem-Ozdemir D.
dc.contributor.authorAtlihan-Gundogdu E.
dc.contributor.authorEkinci M.
dc.contributor.authorHalay E.
dc.contributor.authorAy K.
dc.contributor.authorKarayildirim T.
dc.contributor.authorAsikoglu M.
dc.date.accessioned2024-07-22T08:08:22Z
dc.date.available2024-07-22T08:08:22Z
dc.date.issued2019
dc.description.abstractThe clinical impact and accessibility of 99mTc tracers for cancer diagnosis would be greatly enhanced by the availability of a new, simple, and easy labeling process and radiopharmaceuticals. 5-Fluorouracil is an antitumor drug, which has played an important role for the treatment of breast carcinoma. In the present study, a new derivative of 5-Fluorouracil was synthesized as (1-[{1′-(1′′-deoxy-2′′,3′′:4′′,5′′-di-O-isopropylidene-β-D-fructopyranose-1′′-yl)-1′H-1′,2′, 3′-triazol-4′-yl}methyl]-5-fluorouracil) (E) and radiolabeled with 99mTc. It was analyzed by radio thin layer chromatography for quality control and stability. The radiolabeled complex was subjected to in vitro cell-binding studies to determine healthy and cancer cell affinity using HaCaT and MCF-7 cells, respectively. In addition, in vitro cytotoxicity studies of compound E were performed with HaCaT and MCF-5 cells. The radiochemical purity of the [99mTc]TcE was found to be higher than 90% at room temperature up to 6 hours. The radiolabeled complex showed higher specific binding to MCF-7 cells than HaCaT cells. IC50 values of E were found 31.5 ± 3.4 μM and 20.7 ± 2.77 μM for MCF-7 and HaCaT cells, respectively. The results demonstrated the potential of a new radiolabeled E with 99mTc has selective for breast cancer cells. © 2019 John Wiley & Sons, Ltd.
dc.identifier.DOI-ID10.1002/jlcr.3804
dc.identifier.issn03624803
dc.identifier.urihttp://akademikarsiv.cbu.edu.tr:4000/handle/123456789/14366
dc.language.isoEnglish
dc.publisherJohn Wiley and Sons Ltd
dc.subject1 [[1' (1'' deoxy 2'',3'':4'',5'' di o isopropylidene beta dextro fructopyranose 1'' yl) 1'h 1',2', 3' triazol 4' yl]methyl] 5 fluorouracil tc 99m
dc.subjectcytotoxic agent
dc.subjectfluorouracil derivative
dc.subjectradiopharmaceutical agent
dc.subjectreducing agent
dc.subjectunclassified drug
dc.subjectArticle
dc.subjectcell culture
dc.subjectcell viability
dc.subjectdrug cytotoxicity
dc.subjectdrug synthesis
dc.subjectHaCat cell line
dc.subjecthuman
dc.subjecthuman cell
dc.subjectIC50
dc.subjectin vitro study
dc.subjectisotope labeling
dc.subjectMCF-7 cell line
dc.subjectpH
dc.subjectradioactive thin layer chromatography
dc.subjectradioactivity
dc.subjectradiochemistry
dc.subjectthin layer chromatography
dc.subjecttransepithelial electrical resistance
dc.subjecttransepithelial resistance
dc.titleRadiolabeling and in vitro evaluation of a new 5-fluorouracil derivative with cell culture studies
dc.typeArticle

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