Synthesis, characterization and in vitro biological activity studies of Cu–M (M = Cu 2+, Co 2+, Ni 2+, Mn 2+, Zn 2+) bimetallic complexes

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 pBS (SK−) DNA at a concentrati...

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Veröffentlicht in:European journal of medicinal chemistry 2006-12, Vol.41 (12), p.1494-1503
Hauptverfasser: Rupesh, K.R., Deepalatha, S., Krishnaveni, M., Venkatesan, R., Jayachandran, S.
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container_end_page 1503
container_issue 12
container_start_page 1494
container_title European journal of medicinal chemistry
container_volume 41
creator Rupesh, K.R.
Deepalatha, S.
Krishnaveni, M.
Venkatesan, R.
Jayachandran, S.
description 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 pBS (SK−) DNA at a concentration of 10 μM; however, even at lower concentrations of 2 μM and 0.1 μM, 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 ( I, Ia) showed 50% inhibition of COX-1 and COX-2 activities at as low a concentration as 12.5 μM, 13.5 μM, 14 μM and 14.5 μM. 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 μM concentration. Complexes I and Ia exhibited good anti-microbial activities against all human pathogens tested except Klebsiella pneumoniae. The following studies showed that among the synthesized bimetallic complexes, complexes I and Ia seem to be promising candidates possessing DNA cleavage activities besides anti-microbial and anti-inflammatory properties to serve as chemical nucleases and chemotherapeutic agents. [Display omitted]
doi_str_mv 10.1016/j.ejmech.2005.11.016
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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 pBS (SK−) DNA at a concentration of 10 μM; however, even at lower concentrations of 2 μM and 0.1 μM, 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 ( I, Ia) showed 50% inhibition of COX-1 and COX-2 activities at as low a concentration as 12.5 μM, 13.5 μM, 14 μM and 14.5 μM. 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 μM concentration. Complexes I and Ia exhibited good anti-microbial activities against all human pathogens tested except Klebsiella pneumoniae. The following studies showed that among the synthesized bimetallic complexes, complexes I and Ia seem to be promising candidates possessing DNA cleavage activities besides anti-microbial and anti-inflammatory properties to serve as chemical nucleases and chemotherapeutic agents. [Display omitted]</description><identifier>ISSN: 0223-5234</identifier><identifier>EISSN: 1768-3254</identifier><identifier>DOI: 10.1016/j.ejmech.2005.11.016</identifier><identifier>PMID: 17011670</identifier><identifier>CODEN: EJMCA5</identifier><language>eng</language><publisher>Oxford: Elsevier Masson SAS</publisher><subject>Anti-Bacterial Agents - pharmacology ; Anti-microbial ; Antibiotics. Antiinfectious agents. 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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 pBS (SK−) DNA at a concentration of 10 μM; however, even at lower concentrations of 2 μM and 0.1 μM, 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 ( I, Ia) showed 50% inhibition of COX-1 and COX-2 activities at as low a concentration as 12.5 μM, 13.5 μM, 14 μM and 14.5 μM. 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 μM concentration. Complexes I and Ia exhibited good anti-microbial activities against all human pathogens tested except Klebsiella pneumoniae. The following studies showed that among the synthesized bimetallic complexes, complexes I and Ia seem to be promising candidates possessing DNA cleavage activities besides anti-microbial and anti-inflammatory properties to serve as chemical nucleases and chemotherapeutic agents. [Display omitted]</description><subject>Anti-Bacterial Agents - pharmacology</subject><subject>Anti-microbial</subject><subject>Antibiotics. Antiinfectious agents. Antiparasitic agents</subject><subject>Antifungal Agents - pharmacology</subject><subject>Bimetallic complexes</subject><subject>Biological and medical sciences</subject><subject>COX</subject><subject>Cu(II) complexes</subject><subject>Cyclooxygenase Inhibitors - pharmacology</subject><subject>DNA - drug effects</subject><subject>DNA cleavage</subject><subject>General aspects</subject><subject>Medical sciences</subject><subject>Metals - pharmacology</subject><subject>Models, Molecular</subject><subject>Pharmacology. 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Complexes I and Ia exhibited good anti-microbial activities against all human pathogens tested except Klebsiella pneumoniae. The following studies showed that among the synthesized bimetallic complexes, complexes I and Ia seem to be promising candidates possessing DNA cleavage activities besides anti-microbial and anti-inflammatory properties to serve as chemical nucleases and chemotherapeutic agents. [Display omitted]</abstract><cop>Oxford</cop><pub>Elsevier Masson SAS</pub><pmid>17011670</pmid><doi>10.1016/j.ejmech.2005.11.016</doi><tpages>10</tpages></addata></record>
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subjects Anti-Bacterial Agents - pharmacology
Anti-microbial
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antifungal Agents - pharmacology
Bimetallic complexes
Biological and medical sciences
COX
Cu(II) complexes
Cyclooxygenase Inhibitors - pharmacology
DNA - drug effects
DNA cleavage
General aspects
Medical sciences
Metals - pharmacology
Models, Molecular
Pharmacology. Drug treatments
Spectrometry, Fluorescence
Topoisomerase I Inhibitors
title Synthesis, characterization and in vitro biological activity studies of Cu–M (M = Cu 2+, Co 2+, Ni 2+, Mn 2+, Zn 2+) bimetallic complexes
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