One-Step, Rapid, 18F–19F Isotopic Exchange Radiolabeling of Difluoro-dioxaborinins: Substituent Effect on Stability and In Vivo Applications

Feifei  An; Fuad  Nurili; Haluk  SaymanZahide  OzerHuseyin  CakirogluOmer  ArasRichard  Ting

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One-Step, Rapid, 18F–19F Isotopic Exchange Radiolabeling of Difluoro-dioxaborinins: Substituent Effect on Stability and In Vivo Applications

机译：One-Step, Rapid, 18F–19F Isotopic Exchange Radiolabeling of Difluoro-dioxaborinins: Substituent Effect on Stability and In Vivo Applications

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The β-diketone moiety is commonly present in many anticancer drugs, antibiotics, and natural products. We describe a general method for radiolabeling β-diketone-bearing molecules with fluoride-18. Radiolabeling was carried out via ~(18)F–~(19)F isotopic exchange on nonradioactive difluoro-dioxaborinins, which were generated by minimally modifying the β-diketone as a difluoroborate. Radiochemistry was one-step, rapid ( 80%) and proceeded at room temperature to accommodate the half-life of F-18 (t _(1/2) = 110 min). High molar activities (7.4 Ci/μmol) were achieved with relatively low starting activities (16.4 mCi). It was found that substituents affected both the solvolytic stability and fluorescence properties of difluoro-dioxaborinins. An F-18 radiolabeled difluoro-dioxaborinin probe that was simultaneously fluorescent showed sufficient stability for in vivo positron emission tomography (PET)/fluorescence imaging in mice, rabbits, and patients. These findings will guide the design of probes with specific PET/fluorescence properties; the development of new PET/fluorescence dual-modality reporters; and accurate in vivo tracking of β-diketone molecules.

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《Journal of Medicinal Chemistry》 |2020年第21期|12693-12706|共14页
作者
Feifei An; Fuad Nurili; Haluk SaymanZahide OzerHuseyin CakirogluOmer ArasRichard Ting;
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Institute of Medical Engineering, Department of Biophysics, School of Basic Medical Science, Health Science Center, Xi’an Jiaotong University;

Department of Radiology, Memorial Sloan Kettering Cancer Center;

Department of Nuclear Medicine, Istanbul University, Cerrahpasa Medical Faculty, FatihDepartment of Radiology, Weill Cornell MedicineMedical and Experimental Research Center, Sakarya University, Medical Faculty;

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正文语种英语
中图分类药学;
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One-Step, Rapid, 18F–19F Isotopic Exchange Radiolabeling of Difluoro-dioxaborinins: Substituent Effect on Stability and In Vivo Applications

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