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首页> 外文期刊>Journal of Inorganic Biochemistry: An Interdisciplinary Journal >Synthesis, characterization and binding with DNA of four planaramineplatinum(II) complexes of the forms: trans-PtL2Cl2 and [PtL3Cl]Cl, where L=3-hydroxypyridine, 4-hydroxypyridine and imidazo(1,2-alpha)pyridine
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Synthesis, characterization and binding with DNA of four planaramineplatinum(II) complexes of the forms: trans-PtL2Cl2 and [PtL3Cl]Cl, where L=3-hydroxypyridine, 4-hydroxypyridine and imidazo(1,2-alpha)pyridine

机译：四种形式为：反式PtL2Cl2和[PtL3Cl] Cl的平面胺铂（II）配合物的合成，表征和与DNA的结合，其中L = 3-羟基吡啶，4-羟基吡啶和咪唑并（1,2-α）吡啶

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Four new trans-planaramineplatinum(II) complexes, three of the form: trans-PtCl2L2, code named CH1, CH2 and CH4 where L = 3-hydroxypyridine, 4-hydroxypyridine and imidazo[1,2-alpha]pyridine, respectively, and one of the form: PtClL3, code named CH3 where L = 3-hydroxypyridine, have been prepared and characterized by elemental analyses and IR, Raman, mass and H-1 NMR spectral studies. The interactions of the compounds with salmon sperm and pBR322 plasmid DNAs have been investigated and their activity against human ovarian cancer cell lines: A2780, A2780(cisR) and A2780(ZD0473R) have also been determined. The compounds are believed to form mainly monofunctional N7(G) and bifunctional intrastrand N7(G)N7(G) adducts with DNA, causing a local distortion of DNA as a result of which gel mobility of the DNA changes. The compound containing three planaramine ligands per molecule (CH3) is found to be less reactive than the compounds containing two planaramine ligands per molecule (CH1, CH2 and CH4), which in turn are less reactive than compounds containing one of the same planaramine ligands per molecule. The decrease in reactivity is reflected in lower molar conductivity values (indicating lower degree of dissociation), less pronounced changes caused to DNA conformation (indicating decreased level of platinum-DNA binding) and lower activity. The decreased reactivity of the compounds is due to a greater steric crowding produced by the bulky planaramine ligands. Changes in DNA conformation are also found to be a function of the actual nature of the planaramine ligand. The results illustrate structure-activity relationship. (c) 2005 Elsevier Inc. All rights reserved.
机译：四种新的反式平面胺铂（II）配合物，三种形式：反式-PtCl2L2，代号为CH1，CH2和CH4，其中L分别为3-羟基吡啶，4-羟基吡啶和咪唑并[1,2-α]吡啶，以及一种形式是：PtClL3，代号为CH3，其中L = 3-羟基吡啶，已经制备并通过元素分析和IR，拉曼，质量和H-1 NMR光谱研究表征。研究了化合物与鲑鱼精子和pBR322质粒DNA的相互作用，并确定了它们对人卵巢癌细胞系A2780，A2780（cisR）和A2780（ZD0473R）的活性。据信这些化合物主要与DNA形成单官能的N7（G）和双官能的内链N7（G）N7（G）加合物，导致DNA的局部变形，其结果是DNA的凝胶迁移率改变。发现每个分子中包含三个平面胺配体的化合物（CH3）的反应性比每个分子中包含两个平面胺配体（CH1，CH2和CH4）的化合物的反应性低，而每个分子中包含两个平面胺配体的化合物的反应性则低于每个分子中包含相同平面胺配体的化合物分子。反应性的降低反映在较低的摩尔电导率值（表明较低的解离度），对DNA构象造成的不太明显的变化（表明铂-DNA结合水平降低）和较低的活性上。化合物的反应性降低是由于笨重的平面胺配体产生了更大的空间拥挤。还发现DNA构象的变化是平面胺配体的实际性质的函数。结果说明了结构-活性关系。 （c）2005 Elsevier Inc.保留所有权利。

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