本工作设计合成了6种新型混胺羧酸根合铂(Ⅱ)类配合物[Pt((CH3/CH3NH)(NH3)X2](a～f){其中,X=CH3COO-(乙酸根),CH2CL COO-(氯乙酸根),CHCl2COO-(二氯乙酸根),C6H5-COO-(苯甲酸根),p-CH3-C6H4-COO-(对甲基苯甲酸根),p-CH3O-C6H4-COO-(对甲氧基苯甲酸根)}.通过元素分析、摩尔电导、差热分析、红外光谱、紫外光谱和1H核磁共振谱对配合物进行了表征.通过MTT法研究了配合物的体外抗肿瘤活性,通过等离子体质谱研究了配合物与细胞DNA的键合量;体外抗肿瘤活性测试表明,配合物(a～F)对所测试的肿瘤细胞MCF-7、HCT-8和BGC-823没有表现出活性,但对EJ和HL-60两种肿瘤细胞表现出好的活性,而且配合物(d～f)对HL-60细胞的活性与顺铂相当.配合物(a～f)与HL-60细胞的DNA键合量与其作用浓度表现出一定的依赖性,从小到大的顺序为:cisplatin＜c＜b＜a＜f＜e＜d.%Six new ammine/dimethylamine platinum(Ⅱ)complexes with earboxylates(a～f)have been synthesized and characterized by elemental analysis,conductivity,thermal analysis,IR,UV,and1 H NMR techniques.The cytotoxicity of the complexes was tested by MTT(3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide)assay.The levels of total platinum bound to DNA were measured by ICP-MS.The results show that the complexes(a～f)have selectivity against tested carcinomas,have no cytotoxicity against HCT-8,BGC-823 and MCF7,but have better cytotoxicity against EJ and HL-60,moreover,cytotoxicity of complexes(d～f)against HL-60 is similar to that of cisplatin.The levels of total platinum bound to DNA in HL-60 are increased with increasing concentrations,and the levels of total platinum bound to DNA increase in the following sequence:cisplatin＜C＜b＜a＜f＜e＜d.
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