Synthesis And Structure Of Copper(Ⅱ) Complexes With DNA-binding, BSA-binding Property And In Vitro Anticancer Activity

Cis-platin binds with DNA by covalent bond and inhibits the duplication of DNA. Sincecis-platin successfully applicates in clinic, studies on the design and exploitation of new metalcomplexes with antitumor activities have been hot spots in the filed of inorganic medicinalchemistry. Investigation of the interaction between metal complexes and DNA and BSA play animportant role in investigating of novel antitumor or anticancer drugs. In order to explore neweffective anticancer drugs that could selectively inhibit tumor cells, four polynuclear complexeswith two N,N’-disubstituted oxamides as the ligands have been designed and synthesized, and theircrystal structures, DNA-binding properties, BSA-binding properties and citotoxities also have beenstudied systematically. The detailed contents include several aspects as follows:1. Synthesis and structures of polynuclear complexes: one mononuclear complex wassynthesized and characterized as [Cu(bpy)2(pic)](pic)(1). Three complexes were synthesized andcharacterized by choosing N,N’-bis(N,N’-diethylpropanediamine) as the bridging ligands, including[Cu2(deap)(N3)2]n(2),[Cu2(deap)(bpy)2](ClO4)2(3), Cu2(deap)(SCN)2(4). Their structures havebeen characterized by elemental analyses, IR and single-crystal X-ray diffraction.2. Interactions of complexes with DNA and BSA: the DNA-binding properties of thecomplexes have been studied by the electronic and fluorescence spectra, electrochemicalmeasurements and viscosity measurements. Furthermore, the protein binding ability has beenmonitored by using UV absorption and tryptophan fluorescence quenching experiment in thepresence of the four complexes using bovine serum albumin (BSA) as model protein.3. In vitro citotoxities activities of complexes: The in vitro citotoxities of complexes (1)-(4)against three cancer cell lines: human hepatocellular carcinoma cell line SMMC-7721, humanhepatocellular carcinoma cell Hep G2and human lung adenocarcinoma cell line A549were testedby SRB method, the results indicate that all of the complexes have a certain cytotoxicities againstSMMC-7721,Hep G2and A549cell lines, with IC50values less than100μg/mL, respectively.4. Interactions of Carbamazepine with BSA in the presence of several metal ion: Theinteractions between protein and Carbamazepine has been monitored by using tryptophanfluorescence quenching experiment in the presence of several metal ion using bovine serumalbumin (BSA) as model protein.The researches of this dissertation enrich the content of oxamide-bridged polynuclearcomplexes, supply the chemical basis to explore novel bridging polynuclear complexes with highactivity, low toxicity and antitumor activities, and could be the valuable references for studying the relationship between structures and properties of complexes.