Radiosynthesis and micro-SPECT analysis of triazole-based RGD integrin ligands as non-peptide molecular imaging probes for angiogenesis. Issue 5 (1st March 2015)

• Record Type: Journal Article
• Authors: Bianchini, Francesca; Fabbrizzi, Pierangelo; Menchi, Gloria; Raspanti, Silvia; Bottoncetti, Anna; Passeri, Alessandro; Andreucci, Elena; Guarna, Antonio; Calorini, Lido; Pupi, Alberto; Trabocchi, Andrea
• Is Part Of: Bioorganic & medicinal chemistry. Volume 23:Issue 5(2015)
• Page Start: 1112
• Page End: 1122
• Publication Date: 2015-03-01
• Subjects: Integrins -- Molecular imaging -- Cancer -- Angiogenesis -- Amino acids; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; Biochemistry -- Periodicals; Chemistry, Clinical -- Periodicals; Chemistry, Organic -- Periodicals; Chimie bio-organique -- Périodiques; Chimie pharmaceutique -- Périodiques; 615.19
• DOI: 10.1016/j.bmc.2014.12.065
• Languages: English
• ISSNs: 0968-0896

Abstract

Graphical abstract: Abstract: Taking advantage of click chemistry, we synthesized triazole-containing RGD peptidomimetics capable of binding to αv β3 integrin with diverse potency, and selected 125 I-labeled compounds proved to interact in vitro and in vivo with αv β3 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 αv β3 melanoma xenografts were found using micro-SPECT imaging studies.