2. Academic Validation
  3. Synthesis of carbon-11-labeled casimiroin analogues as new potential PET agents for imaging of quinone reductase 2 and aromatase expression in breast cancer

Synthesis of carbon-11-labeled casimiroin analogues as new potential PET agents for imaging of quinone reductase 2 and aromatase expression in breast cancer

  • Steroids. 2010 Dec;75(12):967-73. doi: 10.1016/j.steroids.2010.06.004.
Min Wang 1,  Mingzhang Gao,  Kathy D Miller,  George W Sledge,  Gary D Hutchins,  Qi-Huang Zheng
Affiliations

Affiliation

  • 1 Department of Radiology and Imaging Sciences, Indiana University School of Medicine, 1345 West 16th Street, L3-208, Indianapolis, IN 46202, USA.
PMID: 20558190 DOI: 10.1016/j.steroids.2010.06.004
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. [(11)C]casimiroin (6-[(11)C]methoxy-9-methyl-[1,3]dioxolo[4,5-h]quinolin-8(9H)-one, [(11)C]11) and its carbon-11-labeled analogues 5,6,8-trimethoxy-1-[(11)C]methyl-4-methylquinolin-2(1H)-one ([(11)C]17), 8-methoxy-1-[(11)C]methyl-4-methylquinolin-2(1H)-one ([(11)C]21a), 6,8-dimethoxy-1-[(11)C]methyl-4-methylquinolin-2(1H)-one ([(11)C]21b), and 5,8-dimethoxy-1-[(11)C]methyl-4-methylquinolin-2(1H)-one ([(11)C]21c), were prepared from their corresponding precursors with [(11)C]methyl triflate ([(11)C]CH(3)OTf) under basic conditions (NaH) through either O- or N-[(11)C]methylation and isolated by semi-preparative HPLC method in 40-50% radiochemical yields decay corrected to end of bombardment (EOB), based on [(11)C]CO(2), and 111-185GBq/mumol specific activity at the end of synthesis (EOS).

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