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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Synthesis, crystal structures, DNA binding and cytotoxicity of two novel platinum(II) complexes containing 2-(hydroxymethyl)pyridine and pyridine-2-carboxylate ligands
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Synthesis, crystal structures, DNA binding and cytotoxicity of two novel platinum(II) complexes containing 2-(hydroxymethyl)pyridine and pyridine-2-carboxylate ligands

机译:含有2-(羟甲基)吡啶和吡啶-2-羧酸酯配体的两种新型铂(II)配合物的合成,晶体结构,DNA结合和细胞毒性

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摘要

Two new platinum(II) complexes, trans-[Pt(2-mpy)2] ·4H2O (1) and [PtCl(2-pyc)(2-hmpy)]·H2O (2), where 2-hmpy = 2-(hydroxymethyl)pyridine, 2-mpy = deprotonated 2-hmpy and 2-pyc = pyridine-2-carboxylate, have been synthesized and characterized by elemental analysis, IR, NMR, and X-ray crystallography. The DNA binding affinities of these complexes for Fish Sperm DNA (FS-DNA) were investigated using fluorescence, viscosity, thermal denaturation and gel electrophoresis measurements. Fluorescence analysis indicates that complex 1 binds to DNA by a single intercalative mechanism, while complex 2 exhibits two types of interactions such as intercalation and covalent binding. Gel electrophoresis assay demonstrates ability of the complexes to cleavage the supercoiled pBR322 plasmid DNA. The in vitro cytotoxicities of both complexes were preliminarily evaluated and the cytotoxicity of complex 1 against the human lung cancer cells (H1299) is similar to oxaliplatin, but higher than transplatin and carboplatin.
机译:两个新的铂(II)配合物,反式[Pt(2-mpy)2]·4H2O(1)和[PtCl(2-pyc)(2-hmpy)]·H2O(2),其中2-hmpy = 2 -(羟甲基)吡啶(2-mpy =去质子化的2-hmpy,2-pyc =吡啶-2-羧酸)已通过元素分析,IR,NMR和X射线晶体学进行了表征。使用荧光,粘度,热变性和凝胶电泳测量研究了这些复合物对鱼精DNA(FS-DNA)的DNA结合亲和力。荧光分析表明,复合物1通过单一插入机制与DNA结合,而复合物2则表现出两种类型的相互作用,例如插入和共价结合。凝胶电泳分析证明了复合物切割超螺旋的pBR322质粒DNA的能力。初步评估了两种复合物的体外细胞毒性,复合物1对人肺癌细胞(H1299)的细胞毒性与奥沙利铂相似,但高于反式铂和卡铂。

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