Improved radiosynthesis of the apoptosis marker 18F-ICMT11 including biological evaluation

Bioorg Med Chem Lett. 2011 Dec 1;21(23):6945-9. doi: 10.1016/j.bmcl.2011.10.001. Epub 2011 Oct 8.

Abstract

We improved the specific radioactivity of the apoptosis imaging isatin derivative (18)F-ICMT11. We then evaluated (18)F-ICMT11 in EL4 tumor-bearing mice 24h after treatment with etoposide/cyclophosphamide combination therapy. Dynamic PET imaging demonstrated increased uptake in the drug-treated (0.115±0.011 SUV) compared to the vehicle-treated EL4 tumors (0.083±0.008 SUV). This effect correlated to the observed increases in apoptotic index.

MeSH terms

  • Animals
  • Apoptosis*
  • Azides / chemical synthesis*
  • Azides / chemistry
  • Biomarkers / chemistry*
  • Diagnostic Imaging
  • Disease Models, Animal
  • Fluorodeoxyglucose F18*
  • Indoles / chemical synthesis*
  • Indoles / chemistry
  • Isatin / chemistry
  • Lymphoma / diagnostic imaging*
  • Mice
  • Molecular Structure
  • Positron-Emission Tomography
  • Radiopharmaceuticals / chemical synthesis*
  • Radiopharmaceuticals / chemistry

Substances

  • (18)F-ICMT11
  • Azides
  • Biomarkers
  • Indoles
  • Radiopharmaceuticals
  • Fluorodeoxyglucose F18
  • Isatin