Synthesis of carbon-11-labeled casimiroin analogues as new potential PET agents for imaging of quinone reductase 2 and aromatase expression in breast cancer |
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Authors: | Min Wang Kathy D. Miller Gary D. Hutchins |
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Affiliation: | a Department of Radiology and Imaging Sciences, Indiana University School of Medicine, 1345 West 16th Street, L3-208, Indianapolis, IN 46202, USA b Department of Medicine, Indiana University School of Medicine, Indianapolis, IN 46202, USA |
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Abstract: | Carbon-11-labeled casimiroin analogues were first designed and synthesized as new potential PET agents for imaging of quinone reductase (QR) 2 and aromatase expression in breast cancer. [11C]casimiroin (6-[11C]methoxy-9-methyl-[1,3]dioxolo[4,5-h]quinolin-8(9H)-one, [11C]11) and its carbon-11-labeled analogues 5,6,8-trimethoxy-1-[11C]methyl-4-methylquinolin-2(1H)-one ([11C]17), 8-methoxy-1-[11C]methyl-4-methylquinolin-2(1H)-one ([11C]21a), 6,8-dimethoxy-1-[11C]methyl-4-methylquinolin-2(1H)-one ([11C]21b), and 5,8-dimethoxy-1-[11C]methyl-4-methylquinolin-2(1H)-one ([11C]21c), were prepared from their corresponding precursors with [11C]methyl triflate ([11C]CH3OTf) under basic conditions (NaH) through either O- or N-[11C]methylation and isolated by semi-preparative HPLC method in 40-50% radiochemical yields decay corrected to end of bombardment (EOB), based on [11C]CO2, and 111-185 GBq/μmol specific activity at the end of synthesis (EOS). |
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Keywords: | Positron emission tomography (PET) Quinone reductase (QR) 2 Aromatase Casimiroin analogues Radiotracers Cancer imaging |
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