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1.
Dalton Trans ; 43(42): 15829-40, 2014 Nov 14.
Artigo em Inglês | MEDLINE | ID: mdl-25223849

RESUMO

Synthesis, spectral, electrochemical and single crystal X-ray diffraction data of a new series of DMSO containing bivalent ruthenium hydrazone complexes are presented. XRD data of two of the new complexes revealed an octahedral coordination around the ruthenium ion satisfied by NOS2Cl2 atoms. Electrochemical studies showed the metal centred, quasi-reversible, one-electron redox behaviour of the new complexes. The binding of these complexes with biomolecules such as calf thymus DNA (CT-DNA) and bovine serum albumin (BSA) protein investigated by different spectrophotometric methods revealed an intercalative mode of interaction. The in vitro cytotoxicity of these complexes evaluated by the MTT assay on a panel of cancer and normal cell lines indicated that the above complexes are more toxic to cancer cells with a few micromolar concentrations as the IC50 value, but are significantly less toxic to normal cell lines. The observed variations in the binding interactions and cytotoxicity of the complexes were attributed to the nature of the hydrazide moiety of the hydrazones that influences their biological activities.


Assuntos
Antineoplásicos , Complexos de Coordenação , Dimetil Sulfóxido , Hidrazonas , Rutênio , Animais , Antineoplásicos/química , Antineoplásicos/farmacologia , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Complexos de Coordenação/química , Complexos de Coordenação/farmacologia , DNA/metabolismo , Dimetil Sulfóxido/química , Dimetil Sulfóxido/farmacologia , Humanos , Hidrazonas/química , Hidrazonas/farmacologia , Camundongos , Células NIH 3T3 , Rutênio/química , Rutênio/farmacologia , Soroalbumina Bovina/metabolismo
2.
Eur J Med Chem ; 78: 281-93, 2014 May 06.
Artigo em Inglês | MEDLINE | ID: mdl-24686015

RESUMO

Two new, binuclear copper(II) hydrazone complexes have been synthesized and characterized by various physico-chemical techniques including single crystal X-ray diffraction. Interaction of these complexes with nucleotide and protein were analyzed by in vitro biochemical and electrochemical analysis. Both the complexes exhibited intercalative mode of binding with DNA. Further, gel electrophoresis assay demonstrated the ability of the complexes to cleave the supercoiled pBR322 plasmid DNA to nicked circular DNA form. Cytotoxicity of the complexes performed against a panel of cancer cell lines and a normal cell line proved that these complexes are potentially cytotoxic against the cancerous cell lines, particularly with IC50 as low as 0.7 µM against HeLa cell line.


Assuntos
Antineoplásicos/farmacologia , Cobre/química , DNA/efeitos dos fármacos , Técnicas Eletroquímicas , Compostos Organometálicos/farmacologia , Albumina Sérica/química , Animais , Antineoplásicos/síntese química , Antineoplásicos/química , Bovinos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Cristalografia por Raios X , DNA/química , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Células HeLa , Humanos , Modelos Moleculares , Estrutura Molecular , Compostos Organometálicos/síntese química , Compostos Organometálicos/química , Relação Estrutura-Atividade
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