4.5 Article

Synthesis and evaluation of N-(2-[18F]fluoro-4-nitrobenzoyl)glucosamine: a preliminary report

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DOI: 10.1007/s10967-010-0935-4

关键词

F-18; Glucosamine; PET; Tumor

资金

  1. National Natural Science Foundation of China [20371009, 20671014, 21071022]
  2. Key laboratory of Radioactive Medicine of Ministry Education
  3. Beijing Municipal Commission of Education

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d-glucosamine at concentration of certain range could kill tumor cells without influencing normal cells. There are also some reports on the antitumor activity of d-glucosamine and its derivatives in murine models. It was therefore postulated that d-glucosamine might have the potential to invade tumor cells. We designed and radiosynthesized a glucosamine derivative, N-(2-[F-18]fluoro-4-nitrobenzoyl)glucosamine ([F-18]FNBG([F-18]7)). Evaluations in vitro and in vivo were performed on tumor bearing mice. Excitingly, the radiochemical purity of [F-18]FNBG([F-18]7) was 99%, and besides the best radiochemical yield was up to 35%. The best T/Bl (Tumor/Blood) and T/M (Tumor/Muscle) ratios of [F-18]FNBG([F-18]7) were 4.40 and 4.84. Although [F-18]FNBG([F-18]7) deserved further studies, the results revealed it might become a potential PET imaging agent for detecting tumors.

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