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 (K_i = 6.1 ± 0.9 nM and 12.4 ± 4.7 nM, respectiv

SUBMITTER: Glaser M 

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

REPOSITORIES: biostudies-literature