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Issue 18, 2009
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Synthesis of functionalised HP-DO3A chelating agents for conjugation to biomolecules

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Abstract

Two novel bifunctional chelating agents (BFCAs) based on the structure of 10-(2-hydroxypropyl)-1,4,7-tetraazacyclododecane-1,4,7-triacetic acid (HP-DO3A) have been designed and synthesized. BFCAs are able to strongly coordinate metals (e.g.Gd(III)) and radiometals (e.g.90Y(III), 177Lu(III) and 111In(III)), and find applications in the synthesis of products for the imaging and treatment of several cancer types. Indeed, these two BFCAs have been employed in solid-phase peptide synthesis (SPPS) and coupled to well-known peptides such as bombesin and RGD analogues in order to target tumor cells. We also report here the conjugation of one of them to Lys8-oxytocin and radiolabeling with 111In(III) to obtain a new radiopharmaceutical product with potential applications in the diagnosis of tumors over-expressing oxytocin receptors.

Graphical abstract: Synthesis of functionalised HP-DO3A chelating agents for conjugation to biomolecules

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Publication details

The article was received on 17 Mar 2009, accepted on 15 Jun 2009 and first published on 20 Jul 2009


Article type: Paper
DOI: 10.1039/B905369G
Org. Biomol. Chem., 2009,7, 3810-3816

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    Synthesis of functionalised HP-DO3A chelating agents for conjugation to biomolecules

    A. Barge, E. Cappelletti, G. Cravotto, A. Ferrigato, L. Lattuada, F. Marinoni and L. Tei, Org. Biomol. Chem., 2009, 7, 3810
    DOI: 10.1039/B905369G

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