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@ARTICLE{Rsler:201263,
      author       = {Rösler, Thomas W. and Matusch, Andreas and Librizzi,
                      Damiano and Arias-Carrión, Oscar and Freundlieb, Nils and
                      Hoeffken, Helmut and Oertel, Wolfgang H. and Depboylu,
                      Candan and Höglinger, Günter U.},
      title        = {{D}iesterified {D}erivatives of
                      5-{I}odo-2′-{D}eoxyuridine as {C}erebral {T}umor
                      {T}racers},
      journal      = {PLoS one},
      volume       = {9},
      number       = {7},
      issn         = {1932-6203},
      address      = {Lawrence, Kan.},
      publisher    = {PLoS},
      reportid     = {FZJ-2015-03568},
      pages        = {e102397},
      year         = {2014},
      abstract     = {With the aim to develop beneficial tracers for cerebral
                      tumors, we tested two novel 5-iodo-2′-deoxyuridine (IUdR)
                      derivatives, diesterified at the deoxyribose residue. The
                      substances were designed to enhance the uptake into brain
                      tumor tissue and to prolong the availability in the
                      organism. We synthesized carrier added
                      5-[125I]iodo-3′,5′-di-O-acetyl-2′-deoxyuridine
                      (Ac2[125I]IUdR),
                      5-[125I]iodo-3′,5′-di-O-pivaloyl-2′-deoxyuridine
                      (Piv2[125I]IUdR) and their respective precursor molecules
                      for the first time. HPLC was used for purification and to
                      determine the specific activities. The iodonucleoside tracer
                      were tested for their stability against human thymidine
                      phosphorylase. DNA integration of each tracer was determined
                      in 2 glioma cell lines (Gl261, CRL2397) and in PC12 cells in
                      vitro. In mice, we measured the relative biodistribution and
                      the tracer uptake in grafted brain tumors. Ac2[125I]IUdR,
                      Piv2[125I]IUdR and [125I]IUdR (control) were prepared with
                      labeling yields of $31–47\%$ and radiochemical purities of
                      $>99\%$ (HPLC). Both diesterified iodonucleoside tracers
                      showed a nearly $100\%$ resistance against degradation by
                      thymidine phosphorylase. Ac2[125I]IUdR and Piv2[125I]IUdR
                      were specifically integrated into the DNA of all tested
                      tumor cell lines but to a less extend than the control
                      [125I]IUdR. In mice, 24 h after i.p. injection, brain
                      radioactivity uptakes were in the following order
                      Piv2[125I]IUdR>Ac2[125I]IUdR>[125I]IUdR. For Ac2[125I]IUdR
                      we detected lower amounts of radioactivities in the thyroid
                      and stomach, suggesting a higher stability toward
                      deiodination. In mice bearing unilateral graft-induced brain
                      tumors, the uptake ratios of tumor-bearing to healthy
                      hemisphere were 51, 68 and 6 for [125I]IUdR, Ac2[125I]IUdR
                      and Piv2[125I]IUdR, respectively. Esterifications of both
                      deoxyribosyl hydroxyl groups of the tumor tracer IUdR lead
                      to advantageous properties regarding uptake into brain tumor
                      tissue and metabolic stability.},
      cin          = {INM-2},
      ddc          = {500},
      cid          = {I:(DE-Juel1)INM-2-20090406},
      pnm          = {333 - Pathophysiological Mechanisms of Neurological and
                      Psychiatric Diseases (POF2-333)},
      pid          = {G:(DE-HGF)POF2-333},
      typ          = {PUB:(DE-HGF)16},
      UT           = {WOS:000341306600072},
      doi          = {10.1371/journal.pone.0102397},
      url          = {https://juser.fz-juelich.de/record/201263},
}