高等学校化学学报 ›› 2011, Vol. 32 ›› Issue (2): 210.

• 研究论文 • 上一篇    下一篇

含甲基咪唑的抗肿瘤转移NAMI-A衍生物的水解和电化学性质

梁曜华1,2,毕葳2,杨滨2, 赵良2, 梁国刚1,2   

  1. 1.  澳门科技大学, 澳门药物及健康应用研究所, 澳门; 
    2.  中国中医科学院中药研究所, 北京100700
  • 收稿日期:2010-08-16 修回日期:2010-12-07 出版日期:2010-02-10 发布日期:2011-02-23
  • 通讯作者: 梁国刚 E-mail:lguogang200@126.com
  • 基金资助:

    澳门科技发展基金(批准号: 012/2009/A1)、 国家科技部国际合作基金(批准号: 2005DFA30990)和中国中医科学院基本科研业务费自主选题项目(批准号: ZZ2006120, Z02089)资助.

Hydrolytic and Electrochemical Property of Antimetastasis NAMI\|A Derivatives Containing Methylimidazole

LIANG Yao-Hua1,2, BI Wei2, YANG Bin2, ZHAO Liang2, LIANG Guo-Gang1,2*   

  1. 1.  Macau Institute for Applied Research in Medicine and Health, Macau University of Science and Technology, Macau, China;
    2.  Institute of Chinese Material Medica, China Academy of Chinese Medical Science, Beijing 100700,  China
  • Received:2010-08-16 Revised:2010-12-07 Online:2010-02-10 Published:2011-02-23
  • Contact: LIANG Guo-Gang E-mail:lguogang200@126.com
  • Supported by:

    澳门科技发展基金(批准号: 012/2009/A1)、 国家科技部国际合作基金(批准号: 2005DFA30990)和中国中医科学院基本科研业务费自主选题项目(批准号: ZZ2006120, Z02089)资助.

摘要: 合成了trans-[RuCl4(DMSO)(4-MeIm)][(4-MeIm)H](4-MeIm=4-甲基咪唑)(化合物1)和trans-[RuCl4(DMSO)(N-MeIm)][(N-MeIm)H](N-MeIm=N-甲基咪唑)(化合物2). 通过UV、NMR、CV研究了配体结构(4-甲基咪唑, N-甲基咪唑)对NAMI-A衍生物的水解机理-动力学、电化学性质及溶液稳定性的影响. 结果表明:化合物1的Ⅰ氯、Ⅱ氯及DMSO水解反应机理与NAMI-A相似, 但其各级水解速率皆比NAMI-A快, 即将推电子的甲基引入咪唑环(4位), 明显加快NAMI-A衍生物的Ⅰ氯、Ⅱ氯及DMSO水解反应速率. 化合物在酸性溶液中的稳定性高于中性溶液.

关键词: 钌配合物, 抗肿瘤转移, 水解动力学, 稳定性

Abstract: trans-[RuCl4(DMSO)(4-MeIm)][(4-MeIm)H].HCl (4-MeIm=4-Methylimidazole, Compd.1) and trans-[RuCl4(DMSO)(N-MeIm)][(N-MeIm)H] (N-MeIm=N-Methylimidazole, Compd.2) were synthesized. The influence of ligand structure (4-MeIm and N-MeIm) on hydrolytic mechanism-kinetics, electrochemical properties and solution stabilities of Ru-NAMI-A derivatives was studied by UV, NMR and cyclic voltammetry. The result shows that the 1st and 2nd chloro-hydrolysis as well as DMSO-hydrolysis mechanisms for two compounds are very similar to that for NAMI-A. However, the hydrolytic rates of Compd. 1 are obviously faster than that of Compd. 2, which means that introducing electron donating group (methyl) into imidazole ring (C4) of NAMI-A would accelerate hydrolytic reaction of Ru-NAMI-A derivatives. The stability of the complexes in acetic buffer solution is much more stable than that of in neural solution.

Key words: Ruthenium complex, Antimetastasis, Hydrolytic kinetics, Stabilities

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