期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 41, 期 12, 页码 1494-1503出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2005.11.016
关键词
Cu(II) complexes; COX; DNA cleavage; bimetallic complexes; anti-microbial
Six new bimetallic complexes of the type CuCu, CuCo, CuNi, CuZn and CuMn were prepared. The structures of these complexes and the ligand have been proposed on the basis of FAB mass, elemental analysis, UV-vis, IR, EPR and CV studies. All the complexes completely cleave C, PBS (SK-) DNA at a concentration of 10 mu M; however, even at lower concentrations of 2 mu M and 0.1 mu M, the complexes (I and Ia) showed partial cleavage. The results of the fluorescence binding studies of the metal complexes with CT-DNA showed that the presence of aliphatic ligands added additional binding effects including electrostatic, hydrogen binding and vander Waals interactions. Complexes (1, Ia) showed 50% inhibition of COX-1 and COX-2 activities at as low a concentration as 12.5 mu M, 13.5 mu M, 14 mu M and 14.5 mu M. Inhibition assay of top I and top II by different complexes in mutant yeast strains (JN394, JN394 t(-1) and JN394 t(2-5)) with all the complexes showed significant inhibition of topoisomerase at 5 mu M concentration. Complexes I and la exhibited good anti-microbial activities against all human pathogens tested except Klebsiella pneunioniae. The following studies showed that among the synthesized bimetallic complexes, complexes I and la seem to be promising candidates possessing DNA cleavage activities besides anti-microbial and anti-inflammatory properties to serve as chemical nucleases and chemotherapeutic agents. (c) 2006 Elsevier Masson SAS. All rights reserved.
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