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首页> 外文期刊>Dalton transactions: An international journal of inorganic chemistry >Copper(ii) complexes with NNO ligands: synthesis, crystal structures, DNA cleavage, and anticancer activities
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Copper(ii) complexes with NNO ligands: synthesis, crystal structures, DNA cleavage, and anticancer activities

机译:铜(II)铜(II)与NNO配体的复合物:合成,晶体结构,DNA裂解和抗癌活性

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摘要

Three novel copper(ii) complexes, Cu(L1)(2) (1), Cu(L2)(2)2DMF (2), and Cu(L3)(2)2DMF (3), were synthesized using three aroylhydrazone ligands, (E)-2-hydroxy-N '-(1-(pyrazin-2-yl)ethylidene)benzohydrazide (HL1), (E)-3-hydroxy-N '-(1-(pyrazin-2-yl)ethylidene)benzohydrazide (HL2) and (E)-4-hydroxy-N '-(1-(pyrazin-2-yl)ethylidene)benzohydrazide (HL3). The complexes were characterized by elemental analysis, infrared (IR), and Ultraviolet-visible light (UV-vis) spectroscopy. The X-ray crystal structures of the complexes all possess a distorted octahedral coordination geometry. Both an absorption spectral titration and a competitive binding assay (ethidium bromide, 4 ',6-diamidino-2-phenylindole (DAPI), and methyl green) revealed that complexes 2 and 3 bind readily to calf thymus DNA (ctDNA) through intercalative and minor groove binding modes. Complexes 2 and 3 also exhibited oxidative cleavage of supercoiled plasmid DNA (pUC19) in the presence of ascorbic acid as an activator. Cytotoxicity studies showed that complexes 2 and 3 possessed high cytotoxicities toward the HeLa human cervical cancer cell line, but weak toxicities toward the L929 normal mouse fibroblast cell line. We therefore have reason to believe that complexes 2 and 3 both show potential as promising anticancer candidate drugs.
机译:三种新型铜(II)配合物,Cu(L1)(2)(1),Cu(L2)(2)2DMF(2)和Cu(L3)(2)2DMF(3)用三种芳酰肼配体合成,合成,(e)-2-羟基-N' - (1-(吡嗪-2-基)亚乙基)苯并酰肼(HL1),(E)-3-羟基-N' - (1-(吡嗪-2-基)亚乙基肼(HL2)和(E)-4-羟基-N' - (1-(吡嗪-2-基)亚乙基)苯并肼(HL 3)。通过元素分析,红外(IR)和紫外线可见光(UV-VI)光谱,该配合物的特征在于。复合物的X射线晶体结构都具有扭曲的八面体配位几何形状。吸收光谱滴定和竞争结合测定(溴化乙锭,4',6-二脒基-2-苯基吲哚(DAPI)和甲基绿)揭示了复合物2和3通过内嵌性和含量粘合到CALF胸腺DNA(CTDNA)结合较小的凹槽绑定模式。复合物2和3还在抗坏血酸作为活化剂存在下表现出超氧化硅脂DNA(PUC19)的氧化切割。细胞毒性研究表明,复合物2和3对Hela人宫颈癌细胞系具有高细胞毒性,但朝向L929正常小鼠成纤维细胞系弱毒性。因此,我们有理由相信复合体2和3都表现为有前途的抗癌候选药物。

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    Guangdong Acad Sci Guangdong Prov Key Lab Microbial Culture Collect State Key Lab Appl Microbiol Southern China Guangdong Inst Microbiol Guangdong Open Lab Appl Guangzhou 510070 Peoples R China;

    Guangdong Acad Sci Guangdong Prov Key Lab Microbial Culture Collect State Key Lab Appl Microbiol Southern China Guangdong Inst Microbiol Guangdong Open Lab Appl Guangzhou 510070 Peoples R China;

    Guangzhou Univ Sch Chem &

    Chem Engn Guangzhou Higher Educ Mega Ctr 230 Wai Huan Xi Rd Guangzhou 510006 Peoples R China;

    Guangdong Acad Sci Guangdong Prov Key Lab Microbial Culture Collect State Key Lab Appl Microbiol Southern China Guangdong Inst Microbiol Guangdong Open Lab Appl Guangzhou 510070 Peoples R China;

    Guangdong Acad Sci Guangdong Prov Key Lab Microbial Culture Collect State Key Lab Appl Microbiol Southern China Guangdong Inst Microbiol Guangdong Open Lab Appl Guangzhou 510070 Peoples R China;

    Guangdong Acad Sci Guangdong Prov Key Lab Microbial Culture Collect State Key Lab Appl Microbiol Southern China Guangdong Inst Microbiol Guangdong Open Lab Appl Guangzhou 510070 Peoples R China;

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  • 正文语种 eng
  • 中图分类 化学;无机化学;
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