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Molecules 2016, 21(3), 387;

Synthesis and Biological Evaluation of an 18Fluorine-Labeled COX Inhibitor—[18F]Fluorooctyl Fenbufen Amide—For Imaging of Brain Tumors

Department of Neurosurgery, Chang-Gung Memorial Hospital at Chiayi and Chang Gung University, Taoyuan 33302, Taiwan
Department of Biomedical Engineering and Environmental Sciences, National Tsinghua University, Hsinchu 300, Taiwan
Department of Surgery, Chang-Gung Memorial Hospital at Linkou and Chang Gung University, Guei-shan 33305,Taiwan
Institute of Nuclear Engineering and Science, National Tsing-Hua University, Hsinchu 300, Taiwan
Author to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 5 February 2016 / Revised: 11 March 2016 / Accepted: 14 March 2016 / Published: 21 March 2016
(This article belongs to the Section Bioorganic Chemistry)
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Molecular imaging of brain tumors remains a great challenge, despite the advances made in imaging technology. An anti-inflammatory compound may be a useful tool for this purpose because there is evidence of inflammatory processes in brain tumor micro-environments. Fluorooctylfenbufen amide (FOFA) was prepared from 8-chlorooctanol via treatment with potassium phthalimide, tosylation with Ts2O, fluorination with KF under phase transfer catalyzed conditions, deprotection using aqueous hydrazine, and coupling with fenbufen. The corresponding radiofluoro product [18F]FOFA, had a final radiochemical yield of 2.81 mCi and was prepared from activated [18F]F (212 mCi) via HPLC purification and concentration. The radiochemical purity was determined to be 99%, and the specific activity was shown to exceed 22 GBq/μmol (EOS) based on decay-corrected calculations. Ex-vivo analysis of [18F]FOFA in plasma using HPLC showed that the agent had a half-life of 15 min. PET scanning showed significant accumulation of [18F]FOFA over tumor loci with reasonable contrast in C6-glioma bearing rats. These results suggest that this molecule is a promising agent for the visualization of brain tumors. Further investigations should focus on tumor micro-environments. View Full-Text
Keywords: Inflammation; molecular imaging; NSAIDs; cyclooxygenase Inflammation; molecular imaging; NSAIDs; cyclooxygenase

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Huang, Y.-C.; Chang, Y.-C.; Yeh, C.-N.; Yu, C.-S. Synthesis and Biological Evaluation of an 18Fluorine-Labeled COX Inhibitor—[18F]Fluorooctyl Fenbufen Amide—For Imaging of Brain Tumors. Molecules 2016, 21, 387.

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