title: 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 αvβ3 integrin with diverse potency, and selected (125)I-labeled compounds proved to interact in vitro and in vivo with αvβ3 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 αvβ3 melanoma xenografts were found using micro-SPECT imaging studies.
authors: Department of Clinical and Experimental Biomedical Science 'Mario Serio', University of Florence, Viale Morgagni 50, 50134 Florence, Italy.
authors: Francesca
authors: F
authors: Bianchini
authors: Department of Chemistry 'Ugo Schiff', University of Florence, Via della Lastruccia 13, 50019 Sesto Fiorentino, Florence, Italy.
authors: Pierangelo
authors: P
authors: Fabbrizzi
authors: Department of Chemistry 'Ugo Schiff', University of Florence, Via della Lastruccia 13, 50019 Sesto Fiorentino, Florence, Italy; Interdepartmental Center for Preclinical Development of Molecular Imaging (CISPIM), University of Florence, Viale Morgagni 85, 50134 Florence, Italy.
authors: Gloria
authors: G
authors: Menchi
authors: Department of Clinical and Experimental Biomedical Science 'Mario Serio', University of Florence, Largo Brambilla 3, 50134 Florence, Italy.
authors: Silvia
authors: S
authors: Raspanti
authors: Azienda Ospedaliera Universitaria Careggi (AOUC), Largo Brambilla 3, 50134 Florence, Italy.
authors: Anna
authors: A
authors: Bottoncetti
authors: Interdepartmental Center for Preclinical Development of Molecular Imaging (CISPIM), University of Florence, Viale Morgagni 85, 50134 Florence, Italy; Department of Clinical and Experimental Biomedical Science 'Mario Serio', University of Florence, Largo Brambilla 3, 50134 Florence, Italy.
authors: Alessandro
authors: A
authors: Passeri
authors: Department of Clinical and Experimental Biomedical Science 'Mario Serio', University of Florence, Viale Morgagni 50, 50134 Florence, Italy.
authors: Elena
authors: E
authors: Andreucci
authors: Department of Chemistry 'Ugo Schiff', University of Florence, Via della Lastruccia 13, 50019 Sesto Fiorentino, Florence, Italy; Interdepartmental Center for Preclinical Development of Molecular Imaging (CISPIM), University of Florence, Viale Morgagni 85, 50134 Florence, Italy.
authors: Antonio
authors: A
authors: Guarna
authors: Department of Clinical and Experimental Biomedical Science 'Mario Serio', University of Florence, Viale Morgagni 50, 50134 Florence, Italy. Electronic address: lido.calorini@unifi.it.
authors: Lido
authors: L
authors: Calorini
authors: Interdepartmental Center for Preclinical Development of Molecular Imaging (CISPIM), University of Florence, Viale Morgagni 85, 50134 Florence, Italy; Department of Clinical and Experimental Biomedical Science 'Mario Serio', University of Florence, Largo Brambilla 3, 50134 Florence, Italy; Azienda Ospedaliera Universitaria Careggi (AOUC), Largo Brambilla 3, 50134 Florence, Italy. Electronic address: a.pupi@dfc.unifi.it.
authors: Alberto
authors: A
authors: Pupi
authors: Department of Chemistry 'Ugo Schiff', University of Florence, Via della Lastruccia 13, 50019 Sesto Fiorentino, Florence, Italy; Interdepartmental Center for Preclinical Development of Molecular Imaging (CISPIM), University of Florence, Viale Morgagni 85, 50134 Florence, Italy. Electronic address: andrea.trabocchi@unifi.it.
authors: Andrea
authors: A
authors: Trabocchi
mesh_terms: D000818:Animals; D064593:Heterografts; D006801:Humans; D016023:Integrins / Q000737:chemistry*; D008024:Ligands; D008545:Melanoma / Q000000981:diagnostic imaging; D051379:Mice; D008958:Models, Molecular; D015335:Molecular Probes; D009389:Neovascularization, Pathologic / Q000175:diagnosis*; D009842:Oligopeptides / Q000138:chemical synthesis / Q000737:chemistry*; D015899:Tomography, Emission-Computed, Single-Photon / Q000379:methods*; D014230:Triazoles / Q000737:chemistry*
chemical_list: D016023:Integrins; D008024:Ligands; D015335:Molecular Probes; D009842:Oligopeptides; D014230:Triazoles; C047981:arginyl-glycyl-aspartic acid
keywords: Amino acids; Angiogenesis; Cancer; Integrins; Molecular imaging