Development of Novel 18F-PET Agents for Tumor Hypoxia Imaging

J Med Chem. 2021 May 13;64(9):5593-5602. doi: 10.1021/acs.jmedchem.0c01962. Epub 2021 Apr 26.

Abstract

Tumor hypoxia is a major factor responsible for tumor progression, metastasis, invasion, and treatment resistance, leading to low local tumor control and recurrence after radiotherapy in cancers. Here,18F-positron emission tomography (PET) probes are developed for visualizing viable hypoxic cells in biopsies. Pimonidazole derivatives and nitroimidazole-based agents bearing sulfonyl linkers were evaluated. A small-animal PET study showed that the tumor uptake of [18F]-23 [poly(ethylene glycols) (PEG)-sulfonyl linker] of 3.36 ± 0.29%ID/g was significantly higher (P < 0.01) than that of [18F]-20 (piperazine-linker tracer, 2.55 ± 0.49%ID/g) at 2 h postinjection in UPPL tumors. The tumor-to-muscle uptake ratio of [18F]-23 (2.46 ± 0.48 at 2 h pi) was well improved compared with that of [18F]-FMISO (1.25 ± 0.14 at 2 h pi). A comparable distribution pattern was observed between ex vivo autoradiography of [18F]-23 and pimonidazole staining of the neighboring slice, indicating that [18F]-23 is a promising PET agent for hypoxia imaging.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Animals
  • Cell Line, Tumor
  • Fluorine Radioisotopes / chemistry
  • Humans
  • Mice
  • Mice, Inbred C57BL
  • Mice, Nude
  • Neoplasms / diagnostic imaging*
  • Nitroimidazoles / chemistry
  • Polyethylene Glycols / chemistry
  • Positron-Emission Tomography
  • Radiopharmaceuticals / chemical synthesis
  • Radiopharmaceuticals / chemistry*
  • Radiopharmaceuticals / metabolism
  • Sulfinic Acids / chemistry
  • Transplantation, Heterologous
  • Tumor Hypoxia*

Substances

  • Fluorine Radioisotopes
  • Nitroimidazoles
  • Radiopharmaceuticals
  • Sulfinic Acids
  • Polyethylene Glycols
  • pimonidazole
  • Fluorine-18