Radiosynthesis and micro-SPECT analysis of triazole-based RGD integrin ligands as non-peptide molecular imaging probes for angiogenesis

Abstract Taking advantage of click chemistry, we synthesized triazole-containing RGD peptidomimetics capable of binding to α v β 3 integrin with diverse potency, and selected 125 I-labeled compounds proved to interact in vitro and in vivo with α v β 3 integrin expressed by melanoma cells. Two 125 I-compounds containing either 2-aminobenzimidazole or 2-aminopyridine groups as the arginine bioisostere with the capacity to selectively bind cells of highly expressing α v β 3 melanoma xenografts were found using micro-SPECT imaging studies.