首页> 外文期刊>BMC Chemical Biology >Studies on the synthesis,characterization,binding with DNA and activities of two cis-planaramineplatinum(II)complexes of the form: cis-PtL(NH3)Cl2 where L=3-hydroxypyridine and 2,3-diaminopyridine
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Studies on the synthesis,characterization,binding with DNA and activities of two cis-planaramineplatinum(II)complexes of the form: cis-PtL(NH3)Cl2 where L=3-hydroxypyridine and 2,3-diaminopyridine

机译:两种形式为L = 3-羟基吡啶和2,3-二氨基吡啶的顺式-PtL(NH3)Cl2的合成,表征,与DNA的结合以及活性的研究

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Background:Cis-planaramineplatinum(II)complexes like their trans isomers are often found to be active against cancer cell lines.The present study deals with the synthesis,characterization and determination of activity of new cis-planaramineplatinum(II)complexes. Results:Two cis-planaramineplatinum(II)complexes:cis-(3- hydroxypyridine)(ammine)dichloroplatinum(II)(code named AH3)and cis-(2,3- diaminopyridine)(ammine)dichloroplatinum(II)(code named AH7)have been prepared and characterised based on elemental analyses,IR,Raman,mass and 1H NMR spectral measurements. The interactions of the compounds with pBR322 plasmid DNA have been investigated and their activity against ovarian cancer cell lines:A2780,A2780cisR and A2780ZD047Rhave been determined. Like cisplatin,AH3 and AH7 are believed to form mainly monofunctional N7(G)and bifunctional intrastrand N7(G)N7(G)adducts with DNA,causing a local distortion of a DNA strand.As a result, gel mobility of the DNA changes.Both AH3 and AH7 are found to be less active than cisplatin against the three cell lines with AH3 being the more active compound of the two.The higher activity of AH3 is in line with its lower molar conductivity value corresponding to a lower degree of dissociation. Conclusion:The differences in activity of AH3,AH7 and cisplatin against the cell lines illustrate structure-activity relationship.
机译:背景:经常发现顺式-平面-氨基铂(II)复合物对癌细胞具有活性。本研究涉及新型顺式-平面-氨基铂(II)复合物的合成,表征和活性测定。结果:两种顺式-平面胺铂(II)配合物:顺式-(3-羟基吡啶)(氨)二氯铂(II)(代号AH3)和顺式(2,3-二氨基吡啶)(氨)二氯铂(II)(代号)已根据元素分析,IR,拉曼,质量和1H NMR光谱测量制备并表征了AH7)。已经研究了化合物与pBR322质粒DNA的相互作用,并且已经确定了它们对卵巢癌细胞系:A2780,A2780cisR和A2780ZD047R的活性。像顺铂一样,AH3和AH7被认为主要与DNA形成单官能N7(G)和双官能内链N7(G)N7(G)加合物,导致DNA链局部变形。结果,DNA的凝胶迁移率发生了变化。发现AH3和AH7在这三种细胞系中的活性均低于顺铂,其中AH3是两者中活性最高的化合物.AH3的较高活性与其较低的摩尔电导率值相对应,即解离度较低。结论:AH3,AH7和顺铂对细胞株活性的差异说明了其构效关系。

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