Radiosynthesis and in vivo tumor uptake of 2-deoxy-2-[18F] fluoro-myo-inositol

Laurence Carroll, Meg Perumal, Neil Vasdev, Edward Robins, Eric O. Aboagye

Research output: Contribution to journalArticle

Abstract

Inositols play an important role in membrane lipid metabolism and mitogenic signaling of most cancer cells. There is paucity of data on the distribution of radiolabelled inositols. Based on work previously carried out on 1-deoxy-1-[18F]fluoro-scyllo-inositol ([18F]2), we began a program of work to label myo-inositol (2-deoxy-2-[18F]fluoro-myo- inositol, [18F]1), the most abundant inositol in cells. Fluorination of a triflate precursor 4 afforded the desired [18F]1 following deprotection with a radiochemical yield of 8% n.d.c. [18F]1 showed higher uptake in vivo in a human breast cancer xenograft model, MDA-MB-231, compared to [18F]2. Thus, we have developed a new inositol radiotracer that could have utility for studying inositol uptake in tumors.

Original languageEnglish (US)
Pages (from-to)6148-6150
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Volume22
Issue number19
DOIs
Publication statusPublished - Oct 1 2012
Externally publishedYes

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Keywords

  • Cancer
  • Fluorine-18
  • Inositol
  • PET Imaging

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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