Synthesis of a kinetically stable yttrium-90 labelled macrocycle–antibody conjugate

Abstract

Lysine is a precursor for the synthesis of an aminobutyl C-functionalised tetra-azacyclododecane tetra-acid which has been linked to 872.3 antibody and may be labelled with 9OY to form a kinetically stable complex of potential use in radio i m mu not h e ra py .

The synthesis, crystal structures and antimicrobial studies of C‐methyl‐substituted hexaaza macrocycle of Cu(II) having aromatic pendant arm

“…The six-membered chelate rings involving the C(8) and C(11) atoms adopted a chair conformation, whereas five-membered rings involving the C(9) and C(12) atoms assumed a gauche conformation. The chelate angles N(1)-Cu-N(2) and N(1)-Cu-N(2)#1 were 94.01(13) and 85.99 (13) • for six-and five-membered rings, respectively. The benzene rings were positioned completely parallel to each other with an interplanar separation of 7.241 (4) Å.…”

“…Extensive reviews on macrocycles have revealed the importance of macrocyclic complexes in biological processes such as photosynthesis and dioxygen transport, [11] catalytic properties, [12] potential applications as metal extractants and as radio-therapeutics. [13] Macrocyclic metal complexes of lanthanides, e.g. Gd(III) and Fe(II), are used as MRI contrast agents.…”

Electrochemical and Spectroscopic Studies on the Interaction between Tetracoordinate Macrocyclic Copper(II), Nickel(II) and Cobalt(III) Complexes with DNA

“…[3][4][5] Studies on these molecules and their transition metal complexes were also focused on application to catalysis, 6 ion selectivity and their use as radioimmunotherapy agents. 7 Due to their importance to biological processes, the synthesis and activity studies of copper(II) and nickel complex have been focused on different respects. [8][9][10] It was reported that copper complexes, including Cu(II) 2 (salicylate) 4 and Cu(II) 2 (3, 4 , might have the potential to inhibit tumor cell growth, and/or cure inflammatory/rheumatic diseases via SOD-mimetic effect.…”

Comparative biodistributions of indium-111-labelled macrocycle chimeric B72.3 antibody conjugates in tumour-bearing mice

“…There has also been considerable interest in the development of macrocycic chelators for the attachment of radioisotopes to antibodies (Moi et al, 1988;Cox et al, 1989;Craig et al, 1989;Deshpande et al, 1990). It has been shown that the macrocycle 1,4,7-triazacyclononanetriacetic acid (termed 9N3) can form very stable complexes with "'In (log KI 26.2/H20, 298KI = 0.1) and the X-ray structure of the indium complex has been solved (Broan et al, 1991).…”

“…In addition, we have developed a series of macrocycic chelators for the attachment of the beta-emitting isotope yttrium-90 to antibodies (Cox et al, 1989). One of these (termed 12N4), has been shown to form stable complexes with 9'Y that have superior biodistribution properties to DTPA and bifunctional DTPA derivatives Harrison et al, 1991).…”