Metal complexes of cyclen and cyclam derivatives useful for medical applications: a discussion based on thermodynamic stability constants and structural data

Delgado, Rita; Félix, Vı́tor; Lima, Luı́s M. P.; Price, David W.

doi:10.1039/b704360k

Cited by 162 publications

(140 citation statements)

References 85 publications

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“…Generally, DOTA forms more stable complexes with lanthanide metal ions, while TETA forms more kinetically stable complexes with transition metal ions [22][23][24]. Especially, DOTA is known to have decreased stability with 64 Cu compared with TETA [20].…”

Section: Introductionmentioning

confidence: 99%

A New Synthesis of TE2A—a Potential Bifunctional Chelator for 64Cu

Pandya

Kim

Kwak

et al. 2010

Nucl Med Mol Imaging

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Purpose The development of a new bifunctional chelator, which holds radiometals strongly in living systems, is a prerequisite for the successful application of diseasespecific biomolecules to medical diagnosis and therapy. Recently, TE2A was reported to make kinetically more stable Cu(II) complexes than TETA. Herein, we report a new synthetic route to TE2A and explore its potential as a bifunctional chelator. Methods TE2A was synthesized using the regioselective alkylation of benzyl bromoacetate and successive deprotection of the methylene bridge and benzyl group. Salt-free TE2A was radiolabeled with 64 Cu and microPET imaging was performed to follow the clearance pattern of the 64 Cu-TE2A complex. TE2A was conjugated with cyclic RGD peptide and the TE2A-c(RGDyK) conjugate was radiolabeled with 64 Cu. Results TE2A was prepared in salt-free form from cyclam in an overall yield of 74%. The microPET images showed that 64 Cu-TE2A is excreted rapidly from the body by the kidney and liver. TE2A was successfully conjugated with c(RGDyK) peptide through one carboxylate group and the TE2A-c(RGDyK) conjugate was radiolabeled with 64 Cu in 94% yield within 30 min. Conclusion TE2A can be used by itself as a bifunctional chelator without any further structural modification.

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Section: Introductionmentioning

confidence: 99%

A New Synthesis of TE2A—a Potential Bifunctional Chelator for 64Cu

Pandya

Kim

Kwak

et al. 2010

Nucl Med Mol Imaging

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“…1,2 The resulting complexes are generally thermodynamically very stable, which has resulted in these systems being used in a range of different applications. 3 For example, coordination of this type of ligand to metals such as 90 Y, 68 Ga and 111 In yields complexes that have been successfully used as radiopharmaceuticals for imaging and therapy. [4][5][6][7][8][9][10] On the other hand, complexes of substituted polyazamacrocycles with lanthanides (e.g.…”

Section: Introductionmentioning

confidence: 99%

Coordination chemistry of amide-functionalised tetraazamacrocycles: structural, relaxometric and cytotoxicity studies

Martinelli

Balali-Mood

Panizzo³

et al. 2010

Dalton Trans.

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Three different tetraazamacrocyclic ligands containing four amide substituents that feature groups (namely allyl, styryl and propargyl groups) suitable for polymerisation have been synthesised. Gadolinium(III) complexes of these three ligands have been prepared as potential monomers for the synthesis of polymeric MRI contrast agents. To assess the potential of these monomers as MRI contrast agents, their relaxation enhancement properties and cytotoxicity have been determined. A europium(III) complex of one of these ligands (with propargyl substituents) is also presented together with its PARACEST properties. In addition, to gain further insight into the coordination chemistry of the tetra-propargyl substitited ligand, the corresponding zinc(II) and cadmium(II) complexes have been prepared.The X-ray crystal structures of the tetra-propargyl ligand and its corresponding gadolinium(III), zinc(II) and cadmium(II) complexes are also presented.

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“…The synthesis of silica supports covalently functionalised with cyclam derivatives has been described [50][51][52][53][54][55][56][57][58][59][60][61]. Cyclams can bind to a range of transition metals, including nickel, often achieving very high thermodynamic and kinetic stability in terms of metal ion dissociation which has lead to applications in catalysis [62] and medicine [63,64]. Ni-cyclam complexes have been extensively studied [65], in particular the tetra-N-substituted complexes [66,67].…”

Section: Immobilisation Of Enzymes By Metal Affinity Methodsmentioning

confidence: 99%

Modification of Mesoporous Silicates for Immobilization of Enzymes

2012

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Mesoporous silicates (MPS) possess ordered pore structures with pore diameters sufficiently large to accommodate a range of enzymes. The successful immobilization of an enzyme on MPS usually requires modification of the surface of MPS to optimize the interactions between the support and the enzyme. Recent developments on the 2 functionalization of MPS for the immobilization of enzymes are described in this review.

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Metal complexes of cyclen and cyclam derivatives useful for medical applications: a discussion based on thermodynamic stability constants and structural data

Cited by 162 publications

References 85 publications

A New Synthesis of TE2A—a Potential Bifunctional Chelator for 64Cu

A New Synthesis of TE2A—a Potential Bifunctional Chelator for 64Cu

Coordination chemistry of amide-functionalised tetraazamacrocycles: structural, relaxometric and cytotoxicity studies

Modification of Mesoporous Silicates for Immobilization of Enzymes

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