title: Syntheses of bifunctional 2,3-diamino propionic acid-based chelators as small and strong tripod ligands for the labelling of biomolecules with (99m)Tc.
abstract: The labelling of targeting biomolecules requires small and hydrophilic complexes in order to not affect the binding properties of the vectors. 2,3-Diamino propionic acid (dap) is a small and strong, albeit scarcely used, tripod ligand for the fac-[(99m)Tc(CO)(3)](+) moiety. We have introduced at the alpha-carbon atom in the basic dap structure various second functionalities such as carboxylato, amino and alpha-amino acid groups via various spacers in order to yield bifunctional chelators. These dap derivatives can be coupled to targeting molecules for application in molecular imaging. Full characterizations of the bifunctional chelators, X-ray structures of intermediates and of one rhenium complex, as well as labelling studies with (99m)Tc, are presented.
authors.affiliation: University of Zürich, Institute of Inorganic Chemistry, Winterthurerstr. 190, 8057 Zürich, Switzerland.
authors.forename: Yu
authors.initials: Y
authors.lastname: Liu
authors.forename: Bruno L
authors.initials: BL
authors.lastname: Oliveira
authors.forename: João D G
authors.initials: JD
authors.lastname: Correia
authors.forename: Isabel C
authors.initials: IC
authors.lastname: Santos
authors.forename: Isabel
authors.initials: I
authors.lastname: Santos
authors.forename: Bernhard
authors.initials: B
authors.lastname: Spingler
authors.forename: Roger
authors.initials: R
authors.lastname: Alberto
mesh_terms: D002614:Chelating Agents / Q000138:chemical synthesis*; D008024:Ligands; D015609:Organotechnetium Compounds / Q000737:chemistry*; D011422:Propionates / Q000737:chemistry*; D013667:Technetium / Q000737:chemistry*
chemical_list: D002614:Chelating Agents; D008024:Ligands; D015609:Organotechnetium Compounds; D011422:Propionates; D013667:Technetium