具有抗癌活性的n-(2-羟基苯氨基)-n′-(3-二乙氨基丙基)草酰胺桥联金属配合物的合成、结构及活性分析-synthesis, structure and activity analysis of n - ( 2 - hydroxyphenylamino ) - n - ( 3 - diethylaminopropyl ) oxalamide bridging metal complexes with anticancer activi.docxVIP

BSA 结合的能力比带有其它端基配体的配合物强；铜配合物与BSA 的结合能力比镍配合物强；4 、 配 合 物 体 外 细 胞 毒 活 性 的 研 究 ： 采 用 SRB 法 研 究 了 配 合 物 (1)-(4) 对 人 肝 癌 细 (SMMC-7721)和人肺腺癌细胞(A549)两种肿瘤细胞株的体外细胞毒活性，发现所测的4个化合 物对SMMC-7721 和A549 都具有不同程度的抑制作用，其半数抑制浓度(IC50)均在100 μg/mL 以下。本论文的研究工作既丰富了草酰胺类配合物的研究内容，为寻找高效、低毒、具有抗肿 瘤活性的新型桥联配合物提供了化学物质基础，又对深入研究配合物的构效关系具有一定的 参考价值。关键词：不对称草酰胺；双核配合物；DNA 相互作用；BSA 相互作用；细胞毒活性Syntheses, Structures and Biological Activities of Metal Complexes Bridged by N-(2-hydroxyphenyl)-N’-[3-(diethyllamino)propyl]oxamide with Antitumor ActivitiesAbstractInvestigations on metal complexes towards DNA and protein are of current interest in connection with information about drug design and tools of molecular biology. Nucleic acid and protein are important target spot of many drugs. Investigation of the interaction between metal complexes towards DNA and protein could obtain important information about the novel antitumor or anticancer drugs design and the mechanism of action of drugs. Oxamides are good candidates as thebridging ligand in forming polynuclear complexes because their coordinating ability toward transition–metal ions can be modified and tuned by changing the nature of the amide. Compared with the extensively researches in symmetrical N,N′-bis(substituted)oxamide polynuclear systems, only few dissymmetrical N,N′-bis-(substituted)oxamide polynuclear complexes have been reported due to the difficulties in their synthesis. In order to explore new effective anticancer drugs that could selectively inhibit tumor cells, in this dissertation, four polynuclear complexes with N-(2-hydroxyphenyl)-N?-[3-(diethyllamino)propyl]oxamide as the ligand have been designed and synthesized, their DNA and BSA-binding properties and antitumor activities also have been studied systematically. The detail contents include several aspects as follows:Synthesis and structures of oxamide bridging complexes: a new oxamido-bridged bicopper(II) complex, [Cu2(pdpox)(bpy)(CH3OH)](ClO4) (1), where H3pdpox and bpy stand for N-(2-hydro