Synthesis, Structures And Bioactivities Of Dna-binding Polynuclear Complexes

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 plays an importantrole in investigating of novel antitumor or anticancer drugs. In order to explore new effectiveanticancer drugs that could selectively inhibit tumor cells, in this dissertation, six polynuclearcomplexes with two N,N’-disubstituted oxamides as the ligands have been designed andsynthesized, and their crystal structures, DNA-binding properties and citotoxities also have beenstudied systematically. The detailed contents include several aspects as follows:1. Synthesis and structures of polynuclear complexes: six complexes were synthesized andcharacterized by choosing N-（2-hydroxyphenyl）-N’-（3-aminopropyl）oxamide （H3papo） andN,N’-bis（N-hydroxyethylaminoethyl）oxamide （H₂heae） as the bridging ligands, including[Cu₂（papo）（bpy）（H₂O）]（NO₃）·H₂O （1）,[Cu₂（papo）（Me2bpy）（NO₃）]·H₂O （2）,[Cu₂（papo）（dabt）（CH₃OH）]（ClO4）（3）,[Cu₂（papo）（dabt）（CH₃CH₂OH）]（pic）（4）,[Cu₂（heae）（tpa）]_n·n（H₂O）（5） and[Cu₄（H₂O）₂（heae）₂（btc）]_n·6nH₂O （6）. Their structures have been characterized by elementalanalyses, IR and single-crystal X-ray diffraction.2. Interactions of complexes with DNA: the DNA-binding properties of the complexes havebeen studied by the electronic and fluorescence spectra, electrochemical measurements andviscosity measurements. Besides, the impacts of terminal ligands and counter-ions on theinteractions between complexes with HS-DNA were also investigated.3. In vitro citotoxities activities of complexes: The in vitro citotoxities of complexes （1）-（6）against two cancer cell lines: human hepatocellular carcinoma cell line SMMC-7721and humanlung adenocarcinoma cell line A549were tested by SRB method, the results indicate that all of thecomplexes have a certain cytotoxicities against SMMC-7721and A549cell lines.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 therelationship between structures and properties of complexes.