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Synthesis, characterization and in vitro cytotoxicity of gold(III) dialkyl/diaryldithiocarbamato complexes

机译:金(III)二烷基/二芳基氨基甲酰胺复合物的合成,表征和体外细胞毒性

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摘要

A series of six dialkyl/diaryldithiocarbamato (dtc) gold(III) complexes 1- 6 of the composition [Au(Me(2)dtc)(2)]Cl (1), [Au(Me(2)dtc)Cl-2] (2), [Au(Et(2)dtc)(2)]Cl (3), [Au(Et(2)dtc)Cl-2] (4), [Au(Bn(2)dtc)(2)]Cl (5), [Au(Bn(2)dtc)Cl-2] (6) (dtc = Dithiocarbamate, Me = Methyl, Et = Ethyl and Bn = Benzyl) was synthesised and characterized by elemental analysis, infrared and NMR spectroscopy, and single crystal X-ray analysis in the case of complexes 4 and 5. The anticancer potential of the complexes was evaluated against MCF7, A2780 and A2780R human cancer cell lines as well as against a healthy MRC5 cell line. The most promising data were obtained for complex 4. It showed similar cytotoxicity as cisplatin against A2780 cells (EC50 approximate to 9.5 mu M vs. EC50 approximate to 10 mu M), and significantly higher cytotoxicity as compared to cisplatin on A2780R and MCF7 cell lines, with EC50 approximate to 2.8 mu M vs. EC50 approximate to 21 mu M, and EC50 approximate to 2.2 mu M vs. EC50 > 50 mu M, respectively. The interactions of the representative complexes 3 and 4 with a mixture of physiological levels of L-cysteine (Cys) and reduced L-glutathione (GSH) were also studied.
机译:一系列6二烷基/ diaryldithiocarbamato(DTC)金(III)的配合物1- 6中的组合物[金(ME(2)DTC)(2)]氯(1),[金(ME(2)DTC)氯离子的2](2),[金(ET(2)DTC)(2)]氯(3),[金(ET(2)DTC)CL-2](4),[金(BN(2)DTC) (2)]段CL(5),[金(BN(2)DTC)CL-2](6)(DTC =二硫代氨基甲酸,Me =甲基,Et =乙基和BN =苄基)的合成和表征通过元素分析,在配合物4和5的配合物的抗肿瘤潜力的情况下红外和NMR光谱,和单晶X射线分析对MCF7,A2780和A2780R人癌细胞系以及对健康的MRC5细胞系进行评估。获得对复杂4.最有前途的数据结果表明相似的细胞毒性如顺铂对A2780细胞(EC 50近似到9.5微米与EC50接近于10微米),以及显著更高的细胞毒性相比,在A2780R和MCF7细胞系顺铂与EC 50近似到2.8微米与EC50 EC50近似到2.2微米与EC50> 50微米,分别近似于21微米,和。代表配合物3和4与L-半胱氨酸(Cys)和降低的L-谷胱甘肽(GSH)的生理水平的混合物之间的相互作用进行了研究。

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  • 来源
    《RSC Advances》 |2015年第99期|共9页
  • 作者单位

    King Fahd Univ Petr &

    Minerals Ctr Res Excellence Nanotechnol CENT Dhahran 31261 Saudi Arabia;

    King Fahd Univ Petr &

    Minerals Dept Chem Dhahran 31261 Saudi Arabia;

    Palacky Univ Fac Sci Div Biol Act Complexes &

    Mol Magnets Reg Ctr Adv Technol &

    Mat CZ-77146 Olomouc Czech Republic;

    Palacky Univ Fac Sci Div Biol Act Complexes &

    Mol Magnets Reg Ctr Adv Technol &

    Mat CZ-77146 Olomouc Czech Republic;

    Palacky Univ Fac Sci Div Biol Act Complexes &

    Mol Magnets Reg Ctr Adv Technol &

    Mat CZ-77146 Olomouc Czech Republic;

    Univ Neuchatel Inst Phys CH-2000 Neuchatel Switzerland;

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  • 正文语种 eng
  • 中图分类 化学;
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