The Synthesis Of Metal Anticancer Drugs With Polypyridyl And Their Antitumor Activity

Four kinds of metal complexes were designed and synthetized. In these metal complexes, phTPY and H2 Bzimpy were selected as ligand, and Cu or Mn was acted as coordinated metal. They were complex 1 [PhTPYCu(Ⅱ)Bzimpy], complex 2 [Ph TPYMn(Ⅱ)Bzimpy], complex 3 [Cu(Ⅱ)(PhTPY)(H2O)]Cl2 and complex 4 [Mn(Ⅱ)(phTPY)(H2O)]Ac2. The crystal structure of complex 1 and complex 2 were characterized by IR, elemental analysis, and X-ray single crystal diffraction, and the result shows that they all belong to monoclinic system with space group P2(1)/C, six-coordination and octahedral geometry; complex 3 and complex 4 were also analysised by elemental analysis and IR in order to deduce their chemical constuction.The interactions of the complexes with calf thymus DNA binding have been investigated by absorption spectroscopy, fluorescence spectroscopy. The spectrophotometric studies showed that the mode of binding of complex 1 and complex 3 could be partial intercalation and their binding constant Kb were 8.0×104 L?mol-1 and 5.12×104 L?mol-1, respectively. The spectrophotometric studies showed the mode of binding of complex 2 could be partial intercalation and electrostatic interaction, and its binding constant Kb was 3.3×104 L?mol-1. The spectrophotometric studies showed that the mode of binding of complex 4 could be intercalation interaction and its binding constant Kb was 8.7×105 L?mol-1, which close to a typical binding constant Kb of [Ru(bpy)2(dppz)]2+.The agarose gel electrophoresis showed that all the four kinds of complexes can cleave circular plasmid pBR322 DNA to both nicked and linear forms when they were irradiated at 310 nm for 15 min.In vitro antiproliferative activities of the four kinds of complexes were studied against human breast carcinoma(MCF-7) and human lung carcinoma(A549) by MTT assay method. The results indicated that all the complexes can effectively inhibit the proliferation. According to the Giemsa dyeing experiment, it was found that the SCF-7 cells were shrinked and the number of adherent cells decreased obviously after action by complex 1 and complexes 2.