RESUMO
Two new complexes, Zn(L)2(H2O)2 (1) and Mn(L)2(H2O)2 (2) [L = 2-Methyl-1H-4,5-imidazoledicarboxylic acid] were synthesized and characterized by elemental analysis, infrared spectroscopy, and single crystal X-ray diffraction. Intramolecular weak interactions, such as hydrogen-bond and intermolecular interactions were presented in the complexes. The activities of the complexes binding with DNA, and cytotoxic activities were studied. The binding of complexes with fish sperm DNA (FS-DNA) was investigated by fluorescence spectra. Gel electrophoresis assay demonstrated the ability of the complexes to cleave the pBR322 plasmid DNA. The cytotoxic activities of the complexes were tested against the KB cell line. Cytotoxic activity studies showed the two complexes exhibited significant cancer cell inhibitory rate. The most active compound was complex 1 with IC50 and CC50value of 36.5, 429, with the selectivity index (SI = 11.75) among the tested compounds.
Assuntos
Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Apoptose/efeitos dos fármacos , Ácidos Carboxílicos/química , DNA/química , Imidazóis/química , Manganês/farmacologia , Compostos Organometálicos/farmacologia , Zinco/farmacologia , Animais , Antineoplásicos/química , Proliferação de Células/efeitos dos fármacos , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Peixes , Humanos , Masculino , Manganês/química , Estrutura Molecular , Compostos Organometálicos/síntese química , Compostos Organometálicos/química , Espermatozoides/química , Relação Estrutura-Atividade , Células Tumorais Cultivadas , Zinco/químicaRESUMO
A series of complexes [Pd(L1)(Phen)]·2H2O (1), [Pd(L2)(Phen)]·H2O (2), [Pd(L3)(Phen)]·H2O (3), [Pd(L4)(Phen)]·2H2O (4) and [Pd(L5)(Phen)]·2H2O (5) were prepared. The complexes were characterized by IR, (1)H NMR, elemental analysis, and single-crystal X-ray diffractometry. The binding of the complexes was investigated by fluorescence spectrum and UV spectrum, showing the ability of interaction with DNA of intercalative mode. Gel electrophoresis assay demonstrated the ability of the complexes to cleave the pBR322 DNA. Moreover, the five complexes bind to DNA with different binding affinities, in ascending order: complex 1 < 2<3 < 4 < 5. Evaluation of cytotoxic activity of the complexes against five different cancer cell lines proved that the complexes exhibited cytotoxic specificity and significant cancer cell inhibitory rate.
