| 顺式-乙二酸-(反式-1,2-二甲胺基环丁烷)合铂(Ⅱ)的合成、表征及抗肿瘤活性 |
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| 引用本文： | 张林涛,丛艳伟,王应飞,陈红娟,刘其星,普绍平. 顺式-乙二酸-(反式-1,2-二甲胺基环丁烷)合铂(Ⅱ)的合成、表征及抗肿瘤活性[J]. 贵金属, 2018, 39(3): 27-32 |
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| 作者姓名： | 张林涛 丛艳伟 王应飞 陈红娟 刘其星 普绍平 |
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| 作者单位： | 昆明贵金属研究所稀贵金属综合利用新技术国家重点实验室;昆明贵研药业有限公司云南省铂族金属抗肿瘤药物工程技术研究中心 |
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| 基金项目： | 云南省科技创新平台建设计划(2016DH008)。 |
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| 摘 要： | 设计并合成了一种洛铂衍生物顺式-乙二酸-(反式-1,2-二甲胺基环丁烷)合铂(Ⅱ)(C8H14O4N2Pt)。采用元素分析、质谱(ESI-MS)、红外光谱(IR)、核磁共振氢谱(1H NMR)对其化学组成和结构进行了确认和表征,用高效液相色谱(HPLC)测定其在水溶液中的稳定性,并用MTS法对其进行抗肿瘤活性评价。结果表明化合物结构与理论一致,在水溶液中比较稳定,对5种常见肿瘤细胞具有明显的抑制作用。
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| 关 键 词： | 药物化学；铂配合物；合成；表征；稳定性；抗癌活性 |
| 收稿时间： | 2017-11-14 |
Synthesis, Characterization and Anticancer Activity of [trans-1,2-bis(aminomethyl)cyclobutane]oxalatoplatinum(II) |
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| ZHANG Lintao,CONG Yanwei,WANG Yingfei,CHEN Hongjuan,LIU Qixing and PU Shaoping. Synthesis, Characterization and Anticancer Activity of [trans-1,2-bis(aminomethyl)cyclobutane]oxalatoplatinum(II)[J]. Precious Metals, 2018, 39(3): 27-32 |
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| Authors: | ZHANG Lintao CONG Yanwei WANG Yingfei CHEN Hongjuan LIU Qixing PU Shaoping |
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| Affiliation: | State Key Laboratory Advanced Technologies of Comprehensive Utilization of Platinum Metals, Kunming Institute of Precious Metals, Kunming 650106, China;Yunnan Engineering and Technology Center of Platinum-based Anti-tumor Drug,Kunming Guiyan Pharmaceutical Co.Ltd., Kunming 650106, China,Yunnan Engineering and Technology Center of Platinum-based Anti-tumor Drug,Kunming Guiyan Pharmaceutical Co.Ltd., Kunming 650106, China,Yunnan Engineering and Technology Center of Platinum-based Anti-tumor Drug,Kunming Guiyan Pharmaceutical Co.Ltd., Kunming 650106, China,Yunnan Engineering and Technology Center of Platinum-based Anti-tumor Drug,Kunming Guiyan Pharmaceutical Co.Ltd., Kunming 650106, China,Yunnan Engineering and Technology Center of Platinum-based Anti-tumor Drug,Kunming Guiyan Pharmaceutical Co.Ltd., Kunming 650106, China and Yunnan Engineering and Technology Center of Platinum-based Anti-tumor Drug,Kunming Guiyan Pharmaceutical Co.Ltd., Kunming 650106, China |
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| Abstract: | A derivative of lobaplatin, [trans-1,2-bis(aminomethyl)cyclobutane]oxalatoplatinum(II), was synthesized and characterized by elemental analysis, ESI-MS, IR and 1H-NMR. The stability in water was measured by HPLC, and the in vitro anticancer activity was tested by MTS method. The results show that the compound is stable in water and exhibits obvious inhibitory effect on 5 tumor cell lines. |
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| Keywords: | medicinal chemistry platinum complexes synthesis characterization stability anticancer activity |
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