首页> 外文期刊>Chemistry: A European journal >Defining the Anti-Cancer Activity of Tricarbonyl Rhenium Complexes: Induction of G2/M Cell Cycle Arrest and Blockade of Aurora-A Kinase Phosphorylation
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Defining the Anti-Cancer Activity of Tricarbonyl Rhenium Complexes: Induction of G2/M Cell Cycle Arrest and Blockade of Aurora-A Kinase Phosphorylation

机译:定义三羰基铼络合物的抗癌活性:诱导G2 / M细胞周期停滞和阻断极光 - 一种激酶磷酸化

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摘要

Rhenium and ruthenium complexes containing N-heterocylic carbene (NHC) ligands and conjugated to indomethacin were prepared. The anticancer properties were probed against pancreatic cell lines, revealing a remarkable activity of the rhenium fragment as anticancer agent. The ruthenium complexes were found to be inactive against the same pancreatic cancer cell lines, either alone or in conjugation with indomethacin. An in-depth biological study revealed the origin of the anticancer properties of the rhenium tricarbonyl fragment, of which a complete elucidation had yet to be achieved. It was found that the rhenium complexes induce cell cycle arrest at the G2/M phase by inhibiting the phosphorylation of Aurora-A kinase. A preliminary study on the structure–activity relationship on a large family of these complexes revealed that the anticancer properties are mainly associated with the lability of the ancillary ligand, with inert complexes showing limited to no anticancer properties.
机译:制备铼和含有N-杂卡配体并缀合与吲哚美辛的钌配合物。 抗癌性质探测胰腺细胞系,揭示了铼片段作为抗癌剂的显着活性。 发现钌配合物在同一胰腺癌细胞系中毫无惰,单独或与吲哚美辛缀合。 深入的生物学研究揭示了铼三羰基片段的抗癌性质的起源,其中尚未实现完全阐明。 发现铼络合物通过抑制极光-N激酶的磷酸化来诱导G2 / M相的细胞周期停滞。 关于这些复合物的大家庭结构 - 活性关系的初步研究表明,抗癌性质主要与辅助配体的可易易脂肪相关,惰性复合物显示限于无抗癌性质。

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  • 来源
    《Chemistry: A European journal》 |2017年第27期|共4页
  • 作者单位

    Curtin Institute of Functional Molecules and Interfaces Department of Chemistry Curtin University Kent Street Bentley 6102 WA (Australia);

    Metabolic Signalling Group School of Biomedical Sciences Curtin Health Innovation Research Institute Curtin University Perth Western Australia 6102 (Australia);

    Metabolic Signalling Group School of Biomedical Sciences Curtin Health Innovation Research Institute Curtin University Perth Western Australia 6102 (Australia);

    School of Chemistry and Biochemistry University of Western Australia Crawley 6009 WA (Australia);

    Metabolic Signalling Group School of Biomedical Sciences Curtin Health Innovation Research Institute Curtin University Perth Western Australia 6102 (Australia);

    Curtin Institute of Functional Molecules and Interfaces Department of Chemistry Curtin University Kent Street Bentley 6102 WA (Australia);

  • 收录信息
  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 应用化学;
  • 关键词

    antitumor agents; cancer; carbenes; Nheterocyclic carbenes; rhenium;

    机译:抗肿瘤剂;癌症;Carbenes;Nhetercyclic carbenes;铼;

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