Andrew S. Craig

The in vivo release of 90Y from cyclic and acyclic ligand-antibody conjugates

Yttrium binding ligands DOTA, caDTPA and CT-DTPA were each conjugated to monoclonal antibody B72.3, labelled with 90Y and injected into mice in order to assess the in vivo inertness of the antibody-linked 90Y-ligand complexes. Levels of 90Y in femur shafts of the DOTA-B72.3 mice were low, being approximately 7 and 44%, respectively, of levels in the femur shafts of the caDTPA-B72.3 and CT-DTPA-B72.3 treated mice. This finding demonstrates the greater inertness and by implication the greater suitability for immunotherapy of the DOTA-90Y complex.

Towards tumour imaging with indium-111 labelled macrocycle–antibody conjugates

C-Functionalised triazacyclododecane and triazacyclononane triacid macrocycles have been covalently attached to a monoclonal antibody and may be labelled with 111In to form kinetically inert radiolabelled complexes.

Synthesis of 1,10-dithia-4,7,13,16-tetra-azacyclo-octadecane, 1-aza-4,7-dithiacyclononane, and N,N′-1,2-bis(1-aza-4,7-dithia-cyclononyl)ethane. Structural and solution studies of their silver complexes

The synthesis of the ligands 1-aza-4,7-dithiacyclononane, N,N′-1,2-bis(1-aza-4,7-dithiacyclo-nonyl)ethane, and 1,10-dithia-4,7,13,16-tetra-azacyclo-octadecane and their silver(I) complexes are reported. Stability constants in water and methanol have been determined using pH-metric methods, and enthalpies of complexation measured calorimetrically in methanol. The N-alkyl derivatives show enhanced enthalpies of complexation, but exhibit unfavourable entropies of complexation. Crystal structures of the [18]-N4S2 and bis[9]-NS2 silver complexes reveal distorted octahedral co-ordination geometry, although in aqueous solution the bis[9]-NS2 silver complex does not adopt the sandwich structure revealed in the crystallographic analysis.

Synthesis of C- and N-functionalised derivatives of 1,4,7-triazacyclononane-1,4,7-triyltriacetic acid (NOTA), 1,4,7,10-tetra-azacyclododecane-1,4,7,10-tetrayltetra-acetic acid (DOTA), and diethylenenetriaminepenta-acetic acid (DTPA): bifunctional complexing agents for the derivatisation of antibodies

Using (2S)-lysine as a precursor, the syntheses of aminobutyl derivatives of 1,4,7-triazacyclononane, 1,4,7,10-tetra-azacyclododecane, and 3-azapentane-1,5-diamine are described. Transformation into their reactive maleimide derivatives is described and alternative strategies for synthesising the title complexing agents involving nitrogen functionalisation are defined.

Crystal and molecular structure of a seven-coordinate chloroindium(III) complex of 1,4,7-triazacyclononanetriacetic acid

Abstract The title macrocyclic ligand forms a seven-coordinate chloroindium complex which exists as a stable neutral hexacoordinate species in aqueous solution.

Preparation and X-ray crystal structure of a silver sandwich complex of an aza-thia macrocycle

Abstract During the course of studies directed towards the synthesis of kinetically stable silver(I) complexes, we have prepared a hexadentate bis-[9]-NS 2 ligand ( 1 ) which may be expected to form a series of stable octahedral complexes with many transition metal ions. The silver(I) complex has been characterized spectroscopically and crystallographically.

Stability, 71Ga NMR, and crystal structure of a neutral gallium(III) complex of 1,4,7-triazacyclononanetriacetate: a potential radiopharmaceutical?

The gallium complex of 1,4,7-triazacyclononanetriacetate is C3-symmetric both in solution and in the solid state and may be observed by 71Ga NMR in aqueous solution in the pH range –0.8 to +12.

Synthesis, solution stability, and crystal structure of aza-thia macrocyclic complexes of silver(I)

The synthesis of the [18]-N4S2 coronand is reported with the crystal structure of the silver complex and determinations of complex stability in both methanol and water.