18 F-labeled analogues of anti-tumor agent calixarene 0118

Calix[4]arene compound 0118 , a topomimetic of the antiangiogenic amphipathic peptide anginex targeting galectin-1, is currently in Phase I clinical trials with terminal cancer patients. Radiolabelled analogues of compound 0118 may serve as a development tool in PK/PD studies of this class of calix[4]arene compounds, and may prove highly valuable for patient stratification and therapy monitoring. So far, such radiotracers have not been described. In this work, we have designed compound 0118 analogues containing a terminal alkyne functional group for introduction of an F-18 label via Cu(I)-catalyzed 1,3-dipolar cycloaddition of 2-[18F]fluoroethylazide.