C-substituted macrocycles as candidates for radioimmunotherapy

P V Bernhardt; P C Sharpe

doi:10.1021/ic000315f

C-substituted macrocycles as candidates for radioimmunotherapy

Inorg Chem. 2000 Sep 4;39(18):4123-9. doi: 10.1021/ic000315f.

Authors

P V Bernhardt¹, P C Sharpe

Affiliation

¹ Department of Chemistry, University of Queensland, Brisbane, 4072, Australia.

PMID: 11198869
DOI: 10.1021/ic000315f

Abstract

The reaction between aryl aldehydes, the macrocyclic ligand 6-methyl-1,4,8,11-tetraazacyclotetradecane-6-amine (L1), and NaBH3CN produces the corresponding benzyl-substituted ligands in good yield. Copper(II) complexes of the ligands derived from salicylaldehyde (L2), p-hydroxybenzaldehyde (L4), and p-carboxybenzaldehyde (L5) were structurally characterized: [CuL2](ClO4)2.3H2O (monoclinic, P2(1)/c, a = 11.915(6) A, b = 13.861(2) A, c = 17.065(8) A, beta = 102.14(2) degrees, Z = 4); [CuL4](ClO4)2 (monoclinic, P2(1)/n, a = 9.550(3) A, b = 17.977(2) A, c = 14.612(4) A, beta 96.76(1) degrees, Z = 4), and [CuL4](ClO4)2 (monoclinic, P2(1)/n, a = 9.286(2) A, b = 11.294(1) A, c = 23.609(8) A, beta 93.68(1) degrees, Z = 4). Conjugation of several CuII complexes to a protein (bovine serum albumin) has been pursued with a view to the application of these macrocycles as bifunctional chelating agents in radioimmunotherapy.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Crystallography, X-Ray
Heterocyclic Compounds / chemistry*
Models, Molecular
Proteins / chemistry
Radioimmunotherapy*

Substances

Heterocyclic Compounds
Proteins