ABSTRACT
In this study, two novel complexes [Cu(MCVH)phen(H(2)O)].ClO(4) (1) and [Cu(MCLH)phen(H(2)O)].ClO(4) (2) (here, MCVH(2)=(7-hydroxy-4-methyl-8-coumarinyl) valine, MCLH(2)=(7-hydroxy-4-methyl-8-coumarinyl) leucine) have been synthesized and characterized by elemental analyses, molar conductance, infrared spectra (IR), (1)H-NMR and UV-Vis measurements. The interactions of them with calf thymus DNA (ct DNA) have been investigated by absorption spectroscopy, fluorescence spectroscopy, circular dichroism spectroscopy and viscosity measurements. Experimental results reveal an intercalative interaction with DNA for the complexes, furthermore the binding affinity of 2 is higher than that of 1 according to the calculated binding constant values. In addition, they were evaluated for their cytotoxic activities toward human prostate cancer cell (PC3), human liver cell (L02) and human myeloid leukemia cancer cell (HL-60) by acid phosphoatase assay. Both of them showed significant cytotoxic potency.
Subject(s)
Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/pharmacology , Coumarins/chemical synthesis , Coumarins/pharmacology , DNA/chemistry , Leucine/analogs & derivatives , Organometallic Compounds/chemical synthesis , Organometallic Compounds/pharmacology , Valine/analogs & derivatives , Animals , Antineoplastic Agents/chemistry , Antineoplastic Agents/toxicity , Binding Sites , Cattle , Cell Line, Tumor , Cell Proliferation/drug effects , Coumarins/chemistry , Coumarins/toxicity , Dose-Response Relationship, Drug , Drug Screening Assays, Antitumor , Humans , Leucine/chemical synthesis , Leucine/chemistry , Leucine/pharmacology , Leucine/toxicity , Ligands , Molecular Structure , Organometallic Compounds/chemistry , Organometallic Compounds/toxicity , Stereoisomerism , Valine/chemical synthesis , Valine/chemistry , Valine/pharmacology , Valine/toxicityABSTRACT
With a bistridentate Schiff-base ligand, N',N'(3)-bis[(1E)-1-(2-pyridinyl)ethylidene)] isophthalohydrazide (H(2)L), a [2x2]G grid complex, [Ni(4)(HL)(4)](ClO(4))(4).4H(2)O.0.5 CH(3)OH (1) has been synthesized and characterized spectroscopically and crystallographically. Spectrometric titrations, ethidium bromide displacement experiments, circular dichroism spectral analysis and viscosity measurements indicate that the compound 1 strongly binds with calf-thymus DNA, presumably via intercalation mechanism. Furthermore, the antioxidant activity (superoxide and hydroxyl radical) of the ligand and its nickel(II) complex is determined by using spectrophotometer methods in vitro. Complex 1 is found to possess potent antioxidant activity and be better than standard antioxidants like mannitol.
