【作者】 黄胜；

【导师】 康杰；

【作者基本信息】 福建医科大学 ， 药物化学， 2011， 硕士

【摘要】 1967年顺铂的首次抗肿瘤活性的发现以及后来的临床应用,使得金属配合物的抗肿瘤活性研究倍受人们的关注。人们不断地设计并且合成出具有新颖结构的有机金属配合物,并进行筛选,希望能从中得到具有高效、低毒、高选择性的抗肿瘤药物。吡啶多羧酸类配体具有多种的配位基团,能以多样方式与金属发生配位作用,因此其配位聚合物的研究也受到学者的广泛关注。1.本文以4‐羟基吡啶2,6‐二甲酸为配体,依据晶体学原理,利用水热法成功合成了以下6个具有多种新颖结构的过渡金属以及稀土金属配位聚合物,并得到了单晶:（1）Nd（CAM）（H₂O）₃·H₂O（2）Cd₄（HCAM）₄（H₂O）₈（3）La₂（CAM）₂（H₂O）₆（4）Sm（CAM）（H₂O）₃H₂O（5）Ce₂（CAM）₂（H₂O）₆（6）Mn——4（CAM）·3H₃O运用X-单晶衍射分析法进行了结构测定,并对配合物晶体结构进行简要的描述。其中配合物（1）与配合物（4）,配合物（3）与配合物（5）为异质同晶。2.测定了红外光谱,对配合物和配体的红外光谱进行了经验归属,对配合物和配体的固体荧光进行简要的性质研究,配体及配合物（1）（2）（3）（4）都表现出荧光特性。3.运用MTT法,检测配合物对K562细胞、HL60细胞的抑制作用,结果表明配合物的抑制作用与浓度呈正相关,只有配合物2对两株细胞均具有一定的细胞毒性作用。而配合物1、6只对HL60细胞表现出活性抑制作用。更多还原

【Abstract】 In 1967, with the discovery and later clinical application of anti-tumor activity of cisplatin, the research on anti-tumor activity of metal coordination compounds had been attracting widely attention. People constantly design and compose organometallic complex compoumds with novel structures, expecting to obtain anticancer drugs with low-toxicity, high-efficiency, and high-selectivity after screening. Pydiyl carboxylate acid ligands with kinds of coordination groups can coordinate to several metal ions with various coordination modes, Therefore their coordination polymers have aroused much interest and become the focus of research.1. In this dissertation, 4-hydroxypyridine-2, 6-dicarboxylic acid was selected as the ligand. Based on the principle of crystallography, six new complexes of transition metal or lanthanide nitrates with novel structures were synthesized by hydrothermal method and obtained in the form of single crystals.（1）Nd（CAM）（H₂O）₃·H₂O（2）Cd₄（HCAM）₄（H₂O）₈（3）La₂（CAM）₂（H₂O）₆（4）Sm（CAM）（H₂O）₃·H₂O（5）Ce₂（CAM）₂（H₂O）₆（6）Mn₄（CAM）₃·H₃OTheir structures have been analyzed by single-crystal X-ray diffraction, and briefly described. Both complex 1、4 and complex 3、5 are homeomorphy compounds, respectively.2. The complexes and ligand have been characterized by IR. Furthermore the IR have been employed to characterized the above compounds. Then fluorimetric analysis has been used to study on the complexes and ligand. Both the ligand and complexes 1,2,3,4 exhibit luminescence. 3. The inhibition of the complexes against K562 and HL60 cells was determined by MTT assay. The results showed that the concentrations of complexes were positively correlated with inhibitions against K562,HL60 cells. Only complex 2 showed certain extent of inhibition against both two cells. And complexes 1,6 showed inhibition against only HL60 cell.更多还原