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One-Pot Radiosynthesis and Biological Evaluation of a Caspase-3 Selective 5-[123,125I]iodo-1,2,3-triazole derived Isatin SPECT Tracer.


ABSTRACT: 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.

SUBMITTER: Glaser M 

PROVIDER: S-EPMC6917698 | biostudies-literature | 2019 Dec

REPOSITORIES: biostudies-literature

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One-Pot Radiosynthesis and Biological Evaluation of a Caspase-3 Selective 5-[<sup>123,125</sup>I]iodo-1,2,3-triazole derived Isatin SPECT Tracer.

Glaser Matthias M   Rajkumar Vineeth V   Diocou Seckou S   Gendron Thibault T   Yan Ran R   Sin Pak Kwan Brian PKB   Sander Kerstin K   Carroll Laurence L   Pedley R Barbara RB   Aboagye Eric O EO   Witney Timothy H TH   Årstad Erik E  

Scientific reports 20191217 1


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 [<sup>18</sup>F]ICMT11 as a candidate tracer for imaging of apoptosis with SPECT, as well as PET. Labelling with radioiodine (<sup>123,125</sup>I) was ach  ...[more]

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