| 那可丁衍生物合成及其作为微管干扰药物的生物学评估(英文) |
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| 引用本文： | 戴厚玲,郑剑斌,林敏,郑静,周福生,董肖椿,郭磊,刘建文,闻韧.那可丁衍生物合成及其作为微管干扰药物的生物学评估(英文)[J].药学学报,2012(10):1347-1357. |
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| 作者姓名： | 戴厚玲 郑剑斌 林敏 郑静 周福生 董肖椿 郭磊 刘建文 闻韧 |
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| 作者单位： | 华东理工大学药学院,上海市新药设计重点实验室;复旦大学药学院 |
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| 基金项目： | supported by the National Science Foundation of China(21102044);Shanghai Committee of Science and Technology(11DZ2260600) |
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| 摘 要： | 以2-羟基-3-甲氧基苯甲醛为原料,经13步反应合成了26个那可丁衍生物。以HL-60细胞为靶细胞,采用MTT法进行了初步的体外抗肿瘤活性研究。结果表明,大多数化合物对HL-60细胞株显示出较好的抑制活性和对微管聚合的抑制作用。优选出的化合物31对HL-60细胞株以及微管聚合的抑制活性是那可丁的3倍并诱导HL-60细胞在G2/M期累积,这为那可丁及其衍生物的抗肿瘤活性构效关系的研究打下了基础,值得进一步研究。
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| 关 键 词： | 那可丁 微管 细胞毒活性 微管干扰药物 |
Synthesis and biological evaluation of noscapine analogues as microtubule-interfering agents |
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| DAI Hou-ling,ZHENG Jian-bin,LIN Min,ZHENG Jing,ZHOU Fu-sheng,DONG Xiao-chun,GUO Lei,LIU Jian-wen,WEN Ren.Synthesis and biological evaluation of noscapine analogues as microtubule-interfering agents[J].Acta Pharmaceutica Sinica,2012(10):1347-1357. |
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| Authors: | DAI Hou-ling ZHENG Jian-bin LIN Min ZHENG Jing ZHOU Fu-sheng DONG Xiao-chun GUO Lei LIU Jian-wen WEN Ren |
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| Institution: | 1,2(1.Shanghai Key Laboratory of New Drug Design,School of Pharmacy,East China University of Science and Technology,Shanghai 200237,China;2.School of Pharmacy,Fudan University,Shanghai 201203,China) |
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| Abstract: | A series of noscapine analogues have been synthesized via 13-step reaction starting from 2hydroxy-3-methoxybenzaldehyde.Anti-tumor activities of these compounds were evaluated against HL-60 cell lines in vitro by the standard MTT assay.It was found that most of these derivatives showed appreciable inhibitory activity against HL-60 and tubulin polymerization.The results also indicated that the potency of compound 31 is about three times more than that of noscapine against HL-60 cell line and tubulin polymerization.Moreover,it induced a massive accumulation of cells in G 2 /M phase.These results showed noscapine and its derivatives were worth to be intensively studied further. |
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| Keywords: | noscapine tubulin cytotoxic activity microtubule-interfering agent |
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