title: Synthesis and evaluation of (18)F-labeled 4-nitrobenzyl derivatives for imaging tumor hypoxia with positron emission tomography: Comparison of 2-[(18)F]fluoroethyl carbonate and 2-[(18)F]fluoroethyl carbamate.
abstract: Two 4-nitrobenzyl derivatives, 2-fluoroethyl 4-nitrobenzyl carbonate 1 and 4-nitrobenzyl N-2-fluoroethyl carbamate 2, were radiolabeled with (18)F and evaluated for imaging tumor hypoxia with positron emission tomography. Although good tumor uptake was observed for [(18)F]1 and [(18)F]2 (>2.5%ID/g at 3-h post-injection), the tracers cleared slowly from nontarget tissues (>1.5%ID/g) and exhibited extensive defluorination in vivo (>4.0%ID/g for bone). Therefore, [(18)F]1 and [(18)F]2 are not suitable for imaging tumor hypoxia due to suboptimal tumor-to-background contrasts.
authors.affiliation: Department of Molecular Oncology, BC Cancer Agency, Vancouver, BC V5Z 1L3, Canada.
authors.forename: Zhengxing
authors.initials: Z
authors.lastname: Zhang
authors.affiliation: Department of Molecular Oncology, BC Cancer Agency, Vancouver, BC V5Z 1L3, Canada.
authors.forename: Joseph
authors.initials: J
authors.lastname: Lau
authors.affiliation: Department of Molecular Oncology, BC Cancer Agency, Vancouver, BC V5Z 1L3, Canada.
authors.forename: Hsiou-Ting
authors.initials: HT
authors.lastname: Kuo
authors.affiliation: Department of Molecular Oncology, BC Cancer Agency, Vancouver, BC V5Z 1L3, Canada.
authors.forename: Chengcheng
authors.initials: C
authors.lastname: Zhang
authors.affiliation: Department of Molecular Oncology, BC Cancer Agency, Vancouver, BC V5Z 1L3, Canada.
authors.forename: Navjit
authors.initials: N
authors.lastname: Hundal-Jabal
authors.affiliation: Department of Molecular Oncology, BC Cancer Agency, Vancouver, BC V5Z 1L3, Canada.
authors.forename: Nadine
authors.initials: N
authors.lastname: Colpo
authors.affiliation: Department of Molecular Oncology, BC Cancer Agency, Vancouver, BC V5Z 1L3, Canada; Department of Radiology, University of British Columbia, Vancouver, BC V5Z 4E3, Canada.
authors.forename: François
authors.initials: F
authors.lastname: Bénard
authors.affiliation: Department of Molecular Oncology, BC Cancer Agency, Vancouver, BC V5Z 1L3, Canada; Department of Radiology, University of British Columbia, Vancouver, BC V5Z 4E3, Canada. Electronic address: klin@bccrc.ca.
authors.forename: Kuo-Shyan
authors.initials: KS
authors.lastname: Lin
mesh_terms: D000818:Animals; D002219:Carbamates / Q000737:chemistry* / Q000493:pharmacokinetics; D002254:Carbonates / Q000737:chemistry* / Q000493:pharmacokinetics; D045744:Cell Line, Tumor; D003106:Colon / Q000000981:diagnostic imaging; D003110:Colonic Neoplasms / Q000150:complications / Q000000981:diagnostic imaging*; D005462:Fluorine Radioisotopes / Q000737:chemistry* / Q000493:pharmacokinetics; D006801:Humans; D000860:Hypoxia / Q000150:complications / Q000000981:diagnostic imaging*; D051379:Mice; D016513:Mice, SCID; D009578:Nitrobenzenes / Q000737:chemistry* / Q000493:pharmacokinetics; D049268:Positron-Emission Tomography / Q000379:methods*
chemical_list: D002219:Carbamates; D002254:Carbonates; D005462:Fluorine Radioisotopes; D009578:Nitrobenzenes
keywords: 2-Fluoroethanol; 2-Fluoroethylamine; Fluorine-18; Hypoxia; Nitroreductase; Positron emission tomography