烷氧基酸为离去基团的铂(Ⅱ)配合物的体外活性研究(英文)
In vitro Cytotoxicity Study on Platinum(Ⅱ) Complexes with Alkoxycarboxylates as Leaving Groups
作者单位
佟太锋 中国药科大学药学院南京 210009 
刘 霞 南京大学配位化学国家重点实验室南京 210009 
诸海滨 南京大学配位化学国家重点实验室南京 210009 
苟少华 南京大学配位化学国家重点实验室南京 210009 
张奕华 中国药科大学药学院南京 210009 
摘要: 合成了5个以直链和带支链烷氧基乙酸为载体配基的顺铂类配合物,通过红外光谱、核磁共振氢谱和质谱对配合物进行了表征,并测试了化合物对肺腺癌SPC-A1和胃腺癌BGC823的体外抗肿瘤活性。生物活性测试结果表明,配合物的活性与离去基团有很大关系。配合物4(顺-二(异丙氧基乙酸根)·[(1R,2R)-1,2-反式环己二胺]合铂(Ⅱ))在2个细胞系中均显示最高的体外抗肿瘤活性,甚至超过顺铂。
关键词: 铂(Ⅱ)配合物  抗肿瘤活性  烷氧基酸根
基金项目: 
Abstract: Five cisplatin-typed platinum complexes, characteristic of linear and branched alkoxycarboxylates as leaving groups, were synthesized and characterized by infrared, electro-spray ionization MS and 1H NMR spectroscopy. In vitro cytotoxicities of these complexes against SPC-A1 human lung adenocarcinoma and BGC823 human gastric adenocarcinoma cell lines were evaluated. Biological tests reveal that the cytotoxicities of these compounds are highly related to the nature of leaving groups. Complex 4, cis-(trans-1R, 2R-diaminocyclohexane) bis (2-isopropoxyacetate) platinum (Ⅱ), shows the highest cytotoxicity against both cell lines, and its cytotoxicity is higher than that of cisplatin.
Keywords: Pt(Ⅱ) complexes  anti-tumor activity  alkoxycarboxylates
 
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佟太锋,刘 霞,诸海滨,苟少华,张奕华.烷氧基酸为离去基团的铂(Ⅱ)配合物的体外活性研究(英文)[J].无机化学学报,2008,24(6):856-860.
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