Simple synthesis of carbon-11-labeled chromen-4-one derivatives as new potential PET agents for imaging of DNA-dependent protein kinase (DNA-PK) in cancer

Appl Radiat Isot. 2012 Aug;70(8):1558-63. doi: 10.1016/j.apradiso.2012.04.023. Epub 2012 Apr 27.


Carbon-11-labeled chromen-4-one derivatives were synthesized as new potential PET agents for imaging of DNA repair enzyme DNA-dependent protein kinase (DNA-PK) in cancer. The target tracers, X-[(11)C]methoxy-2-morpholino-4H-chromen-4-ones (X=8, 7, 6, 5; [(11)C]4a-d), were prepared from their corresponding precursors, X-hydroxy-2-morpholino-4H-chromen-4-ones (X=8, 7, 6, 5; 5a-d), with [(11)C]CH(3)OTf through O-[(11)C]methylation and isolated by a simplified solid-phase extraction (SPE) method using a C-18 Sep-Pak Plus cartridge. The radiochemical yields decay corrected to end of bombardment (EOB), from [(11)C]CO(2), were 40-60%. The specific activity at end of synthesis (EOS) was 185-370 GBq/μmol.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Benzopyrans / chemical synthesis*
  • Benzopyrans / chemistry
  • Carbon Radioisotopes / chemistry*
  • DNA-Activated Protein Kinase / metabolism*
  • Humans
  • Magnetic Resonance Spectroscopy
  • Neoplasms / enzymology*
  • Positron-Emission Tomography*
  • Spectrometry, Mass, Electrospray Ionization


  • Benzopyrans
  • Carbon Radioisotopes
  • DNA-Activated Protein Kinase