| 萘酰亚胺多胺衍生物的合成及其抗肿瘤活性 |
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| 引用本文： | 罗稳,李展,翟洋洋,谢松强,王超杰.萘酰亚胺多胺衍生物的合成及其抗肿瘤活性[J].应用化学,2013,30(3):0-270. |
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| 作者姓名： | 罗稳 李展 翟洋洋 谢松强 王超杰 |
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| 作者单位： | (河南大学1.天然药物与免疫工程重点实验室；2.化学生物研究所 开封 475004) |
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| 基金项目： | 国家自然科学基金重大研究计划培育项目(90913001) |
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| 摘 要： | 设计合成了萘酰亚胺的4种新的多胺衍生物并进行了体外抗肿瘤活性测试。结果表明,这些萘酰亚胺衍生物能够嵌入DNA碱基对中,并且比氨萘非特对肿瘤细胞具有更高的毒性和更好的选择性,其中化合物3b对4种肿瘤细胞的抑制IC50值分别为7.80、5.08、9.78和9.27μmol/L;高内涵活细胞成像系统结果显示,这些化合物可能是通过线粒体通路而导致的细胞凋亡。
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| 关 键 词： | 萘酰亚胺 DNA嵌入剂 抗肿瘤 高内涵成像 |
| 收稿时间： | 2012-04-19 |
| 修稿时间： | 2012-06-14 |
Synthesis and Antitumor Activity of Polyamine Derivatives of Naphthalimide |
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| LUO Wen
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LI Zhan
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ZHAI Yangyang
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XIE Songqiang
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WANG Chaojie.Synthesis and Antitumor Activity of Polyamine Derivatives of Naphthalimide[J].Chinese Journal of Applied Chemistry,2013,30(3):0-270. |
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| Authors: | LUO Wen LI Zhan ZHAI Yangyang XIE Songqiang WANG Chaojie |
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| Institution: | (1.Key Laboratory of Natural Medicine and Immuno-Engineering;2.Institute of Chemical Bioogy,He′nan University,Kaifeng 475004,China) |
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| Abstract: | A series of polyamine derivatives of naphthalimide(3a~3d) to be used as antitumor agents was synthesized. The biological and spectroscopic evaluations showed that compounds 3a~3d could used as DNA intercalators and had stronger cytotoxic activity and better selectivity than those of amonafide against cancer cells in vitro. The IC50 for antiproliferative activity of compound 3b on four cancer cells were 7.80, 5.08, 9.78 and 9.27 μmol/L, respectively. High content screening(HCS) results revealed that the as-prepared compounds might produce cytotoxicity through apoptosis via mitochondrial pathway. |
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| Keywords: | Naphthalimide DNA intercalator antitumor High Content Screening |
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