4.6 Article

Synthesis and in vivo stability studies of [18F]-zwitterionic phosphonium aryltrifluoroborate/indomethacin conjugates

Journal

RSC ADVANCES
Volume 6, Issue 28, Pages 23126-23133

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/c5ra26323a

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Funding

  1. Cancer Prevention Research Institute of Texas [RP130604]
  2. National Institute of Biomedical Imaging and Bioengineering [1R01EB014354-01A1]
  3. National Cancer Institute [P30-CA016086-35-37]
  4. Biomedical Research Imaging Center, University of North Carolina at Chapel Hill
  5. Development and Promotion of Science and Technology (DPST) project under Royal Thai Government

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With the goal of developing new positron emission tomography (PET) probes for imaging inflammation in cancer tumours, we have conjugated zwitterionic phosphonium aryltrifluoroborates as fluoride captors with indomethacin, a known cyclooxygenase 2 inhibitor. The resulting conjugates have been radiolabeled by F-18-F-19 isotopic exchange in aqueous solutions. NMR studies combined with in vivo data show that the nature of the phosphonium substituents plays an important role on the stability of the radiotracers.

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