This paper reports the synthesis and characterization of bimodal mechanically interlocked rotaxane-based imaging agents for targeting cancer biomarkers. Two synthetic routes, involving four- or six-component reactions, are developed to access asymmetric rotaxanes. A peptide-based rotaxane, targeted toward the prostate cancer biomarker PSMA and bearing a ⁶⁸Ga-radiometal ion complex for PET and fluorescein for OFI, was synthesized. In vitro studies demonstrated the viability of this asymmetric rotaxane platform for producing dual-modality imaging agents that specifically target prostate cancer cells.

Faustine d'Orchymont, Jason P. Holland