Looking for a PET Tracer for Imaging Apoptosis

In multicellular organisms, homeostasis is maintained by a balance between cell proliferation and apoptosis (programmed cell death). It is a physiological form of cell death responsible for the deletion of non-repairable damaged, mutated, or cells which have lost their function.

We describe the synthesis of a series of potential inhibitors of caspases from a modified aspartic acid residue (fluoromethylketone, fmk). The addition to the entire series of, 3-cyano-4-fluoro-benzoyl- pattern on one hand or of, 4-fluoro-2-thiazolamino- pattern on the other hand will subsequently allow the introduction of a PET isotope (¹⁸F).

In order to determine potential candidates, the inhibitory activity of these compounds was evaluated in vitro on a series of human T cells compared to the z-VAD-fmk as a reference.