title: Radiosynthesis and in vivo tumor uptake of 2-deoxy-2-[(18)F]fluoro-myo-inositol.
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-[(18)F]fluoro-scyllo-inositol ([(18)F]2), we began a program of work to label myo-inositol (2-deoxy-2-[(18)F]fluoro-myo-inositol, [(18)F]1), the most abundant inositol in cells. Fluorination of a triflate precursor 4 afforded the desired [(18)F]1 following deprotection with a radiochemical yield of 8% n.d.c. [(18)F]1 showed higher uptake in vivo in a human breast cancer xenograft model, MDA-MB-231, compared to [(18)F]2. Thus, we have developed a new inositol radiotracer that could have utility for studying inositol uptake in tumors.
authors.affiliation: Comprehensive Cancer Imaging Centre, Department of Surgery and Cancer, Hammersmith Campus, Imperial College, London W12 0NN, UK.
authors.forename: Laurence
authors.initials: L
authors.lastname: Carroll
authors.forename: Meg
authors.initials: M
authors.lastname: Perumal
authors.forename: Neil
authors.initials: N
authors.lastname: Vasdev
authors.forename: Edward
authors.initials: E
authors.lastname: Robins
authors.forename: Eric O
authors.initials: EO
authors.lastname: Aboagye
mesh_terms: D000818:Animals; D001943:Breast Neoplasms / Q000000981:diagnostic imaging* / Q000378:metabolism / Q000473:pathology; D045744:Cell Line, Tumor; D005260:Female; D006801:Humans; D007294:Inositol / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics; D051379:Mice; D009374:Neoplasms, Experimental / Q000000981:diagnostic imaging* / Q000378:metabolism / Q000473:pathology; D011877:Radionuclide Imaging
chemical_list: C577888:2-deoxy-2-((18)F)fluoro-myo-inositol; D007294:Inositol