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.
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.
Department of Radiology and Imaging Sciences, Indiana University School of Medicine, 1345 West 16th Street, L3-202, Indianapolis, IN 46202, USA.
Mingzhang
M
Gao
Min
M
Wang
Kathy D
KD
Miller
Qi-Huang
QH
Zheng
D001578:Benzopyrans / Q000138:chemical synthesis* / Q000737:chemistry; D002250:Carbon Radioisotopes / Q000737:chemistry*; D051747:DNA-Activated Protein Kinase / Q000378:metabolism*; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D009369:Neoplasms / Q000201:enzymology*; D049268:Positron-Emission Tomography; D021241:Spectrometry, Mass, Electrospray Ionization
D001578:Benzopyrans; D002250:Carbon Radioisotopes; D051747:DNA-Activated Protein Kinase