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Publication Detail
One-Pot Radiosynthesis and Biological Evaluation of a Caspase-3 Selective 5-[¹²³,¹²⁵I]iodo-1,2,3-triazole derived Isatin SPECT Tracer.
  • Publication Type:
    Journal article
  • Publication Sub Type:
  • Authors:
    Glaser M, Rajkumar V, Diocou S, Gendron T, Yan R, Sin PKB, Sander K, Carroll L, Pedley RB, Aboagye EO, Witney TH, Årstad E
  • Publisher:
    Nature Publishing Group
  • Publication date:
  • Pagination:
  • Journal:
    Scientific Reports
  • Volume:
  • Issue:
  • Status:
    Published online
  • Country:
  • Print ISSN:
  • PII:
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Induction of apoptosis is often necessary for successful cancer therapy, and the non-invasive monitoring of apoptosis post-therapy could assist in clinical decision making. Isatins are a class of compounds that target activated caspase-3 during apoptosis. Here we report the synthesis of the 5-iodo-1,2,3-triazole (FITI) analog of the PET tracer [18F]ICMT11 as a candidate tracer for imaging of apoptosis with SPECT, as well as PET. Labelling with radioiodine (123,125I) was achieved in 55 ± 12% radiochemical yield through a chelator-accelerated one-pot cycloaddition reaction mediated by copper(I) catalysis. The caspase-3 binding affinity and selectivity of FITI compares favourably to that of [18F]ICMT11 (Ki = 6.1 ± 0.9 nM and 12.4 ± 4.7 nM, respectively). In biodistribution studies, etoposide-induced cell death in a SW1222 xenograft model resulted in a 2-fold increase in tumour uptake of the tracer. However, the tumour uptake was too low to allow in vivo imaging of apoptosis with SPECT.
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