Iodoazomycin Riboside [l-(5′-iodo-5′- deoxyribofuranosyl)-2-nitroimidazolel, a Hypoxic Cell Marker In Vivo Evaluation in Experimental Tumors

  • L. I. Wiebe
  • D. C. Jette
  • J. D. Chapman
  • R. J. Flanagan
  • B. E. Meeker


Radiosensitizers labelled with nuclides which emit gamma rays have been proposed to have clinical value in the detection of radioresistant hypoxic cell populations in tumors [1]. Such a diagnostic procedure would be of value for radiation and/or chemotherapy treatment planning in oncology, and could aid the study and treatment of ischemic tissue in the myocardium and in the brain. However, the sensitizers 4-[82Br]-bromomisonidazole (BrMISO) [2] and l-[2-(2-[131I]iodophenoxy)-ethyl]-2-nitroimidazole (IPENI) [3] failed to undergo selective uptake in experimental tumor models. In both cases, and especially with IPENI, the test substances were more lipophilic than hypoxic cell markers used previously [4]. Recent efforts with tritiated misonidazole to label hypoxic cell fractions in human tumors have provided clinical data which support the concept that hypoxic cells may be detected by scintigraphic methods [5].


Hypoxic Cell Tissue Distribution Study Experimental Tumor Model Metabolic Trapping Tissue Distribution Data 
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  1. 1.
    Chapman JD, Franko AJ, Sharplin J (1984) A marker for hypoxic cells in tumors with potential clinical applicability. Br J Cancer 43:546CrossRefGoogle Scholar
  2. 2.
    Jette DC, Wiebe LI, Chapman JD (1983) Synthesis and in vivo distribution and metabolism of the radiosensitizer 4-(82Br) bromomisonidazole in tumor-bearing and normal mice. Int J Nucl Med Biol 10:205–210PubMedCrossRefGoogle Scholar
  3. 3.
    Wiebe LI, Jette DC, Chapman JD (1984) Electron-affinic compounds for labelling hypoxic cells: the synthesis and characterization of 1-[2-(2-iodophenoxy)-ethyl]-2-nitroimidazole. Nuklearmedizin 2:63–67Google Scholar
  4. 4.
    Chapman JD, Baer K, Lee J (1983) Characteristics of the metabolism-induced binding of misonidazole to hypoxic mammalian cells. Cancer Res 43:1523–1528PubMedGoogle Scholar
  5. 5.
    Chapman JD et al. Unpublished work in progressGoogle Scholar
  6. 6.
    Jette DC, Wiebe LI, Lee J, Flanagan RJ, Chapman JD (in press) Iodoazomycin riboside [1- (5′-iodo-5′-deoxyribofuranosyl)-2-nitroimidazole], a hypoxic cell marker. 1. In vitro characterization. Rad ResGoogle Scholar
  7. 7.
    Jarvis SM, Chapman JD, Ngan-Lee J, Rutledge KA, Barr PJ, Paterson ARP (1982) Azomycin riboside, a sugar homologue of misonidazole with favorable radiosensitizing properties. Cancer Res 42:4358–4363PubMedGoogle Scholar
  8. 8.
    Moulder JE, Rockwell S (1984) Hypoxic fractions of solid tumors: Experimental techniques, methods of analysis and a survey of existing data. Int J Radiat Oncol Biol Phys 10:695–712PubMedCrossRefGoogle Scholar
  9. 9.
    Thorndyke C, Meeker BE, Thomas G, Lakey WH, McPhee MS, Chapman JD (1985) The radiation sensitivities of R3327-H and R3327-AT rat prostate adenocarcinoma. J Urol 134Google Scholar

Copyright information

© Springer-Verlag Berlin Heidelberg 1986

Authors and Affiliations

  • L. I. Wiebe
    • 1
  • D. C. Jette
  • J. D. Chapman
  • R. J. Flanagan
  • B. E. Meeker
  1. 1.Faculty of Pharmacy and Pharmaceutical SciencesUniversity of AlbertaEdmontonCanada

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