Synthesis of bifunctional chelating agents based on mono and diphosphonic derivatives of diethylenetriaminepentaacetic acid |
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Authors: | Giovanni B. Giovenzana Claudia Guanci Silvia Demattio Luciano Lattuada Veronica Vincenzi |
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Affiliation: | 1. Dipartimento di Scienze del Farmaco, Università degli Studi del Piemonte Orientale “A. Avogadro”, Largo Donegani 2/3, Novara 28100, Italy;2. Bracco Imaging Spa, Bracco Research Centre, Via Ribes 5, Colleretto Giacosa, TO 10010, Italy |
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Abstract: | Bifunctional chelating agents (BFCAs) are small molecules containing a chelating unit, able to strongly coordinate a metal ion, and a reactive functional group, devised to form a stable covalent bond with another molecule. BFCAs are widely employed since their conjugation to a suitable biomolecule (e.g., a peptide or an antibody) allows the synthesis of diagnostic or therapeutic agents that specifically target diseased tissue with metals or radiometals. For this reason, BFCAs find application in diagnostic imaging, molecular imaging, and radiotherapy of cancer. The synthesis of new BFCAs based on a diethylenetriaminepentaacetic acid (DTPA) structure in which one or two carboxylic groups are replaced with phosphonic units is described. The phosphonic group, aside from being a classical isostere of the carboxylic acid in coordination chemistry, allows to modulate the physico-chemical properties of the ligands and of the corresponding complexes. |
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Keywords: | Bifunctional chelating agents Contrast agents Conjugation Metal complexation DTPA |
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