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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 |
Synthesis, Characterization and Anticancer Activity of [trans-1,2-bis(aminomethyl)cyclobutane]oxalatoplatinum(II) |
Received:November 14, 2017 |
DOI: |
中文关键词: 药物化学 铂配合物 合成 表征 稳定性 抗癌活性 |
英文关键词: medicinal chemistry platinum complexes synthesis characterization stability anticancer activity |
基金项目:云南省科技创新平台建设计划(2016DH008)。 |
Author Name | Affiliation | E-mail | ZHANG Lintao | 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 | 344598617@qq.com | CONG Yanwei | Yunnan Engineering and Technology Center of Platinum-based Anti-tumor Drug,Kunming Guiyan Pharmaceutical Co.Ltd., Kunming 650106, China | | WANG Yingfei | Yunnan Engineering and Technology Center of Platinum-based Anti-tumor Drug,Kunming Guiyan Pharmaceutical Co.Ltd., Kunming 650106, China | | CHEN Hongjuan | Yunnan Engineering and Technology Center of Platinum-based Anti-tumor Drug,Kunming Guiyan Pharmaceutical Co.Ltd., Kunming 650106, China | | LIU Qixing | Yunnan Engineering and Technology Center of Platinum-based Anti-tumor Drug,Kunming Guiyan Pharmaceutical Co.Ltd., Kunming 650106, China | | PU Shaoping | Yunnan Engineering and Technology Center of Platinum-based Anti-tumor Drug,Kunming Guiyan Pharmaceutical Co.Ltd., Kunming 650106, China | pushaoping@163.com |
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中文摘要: |
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。 |
英文摘要: |
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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