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

Ilem-Ozdemir, Derya; Atlihan-Gundogdu, Evren; Ekinci, Meliha; Halay, Erkan; Ay, Kadir; Karayildirim, Tamer; Asikoglu, Makbule


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  <dc:creator>Ilem-Ozdemir, Derya</dc:creator>
  <dc:creator>Atlihan-Gundogdu, Evren</dc:creator>
  <dc:creator>Ekinci, Meliha</dc:creator>
  <dc:creator>Halay, Erkan</dc:creator>
  <dc:creator>Ay, Kadir</dc:creator>
  <dc:creator>Karayildirim, Tamer</dc:creator>
  <dc:creator>Asikoglu, Makbule</dc:creator>
  <dc:date>2019-01-01</dc:date>
  <dc:description>The clinical impact and accessibility of Tc-99m 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-beta-D-fructopyranose-1 ''-yl)-1 ' H-1 ',2 ', 3 '-triazol-4 '-yl}methyl]-5-fluorouracil) (E) and radiolabeled with Tc-99m. 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 [Tc-99m]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 mu M and 20.7 +/- 2.77 mu M for MCF-7 and HaCaT cells, respectively. The results demonstrated the potential of a new radiolabeled E with Tc-99m has selective for breast cancer cells.</dc:description>
  <dc:identifier>https://aperta.ulakbim.gov.trrecord/67797</dc:identifier>
  <dc:identifier>oai:zenodo.org:67797</dc:identifier>
  <dc:rights>info:eu-repo/semantics/openAccess</dc:rights>
  <dc:rights>http://www.opendefinition.org/licenses/cc-by</dc:rights>
  <dc:source>JOURNAL OF LABELLED COMPOUNDS &amp; RADIOPHARMACEUTICALS 62(13) 874-884</dc:source>
  <dc:title>Radiolabeling and in vitro evaluation of a new 5-fluorouracil derivative with cell culture studies</dc:title>
  <dc:type>info:eu-repo/semantics/article</dc:type>
  <dc:type>publication-article</dc:type>
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