| N-取代苄基-4-羟基-4-取代哌啶衍生物的合成及初步抗白血病活性 |
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| 引用本文： | 方治坤,薛思佳,陈龙,胥杨,尹安琴,李春炎. N-取代苄基-4-羟基-4-取代哌啶衍生物的合成及初步抗白血病活性[J]. 中国化学, 2009, 27(2): 397-402. DOI: 10.1002/cjoc.200990065 |
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| 作者姓名： | 方治坤 薛思佳 陈龙 胥杨 尹安琴 李春炎 |
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| 作者单位： | (上海师范大学生命与环境科学学院化学系 上海200234) |
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| 摘 要： | 为了寻找对白血病细胞系增殖有较高抑制活性的先导化合物，本文以取代苄胺为原料，经Michael加成，Dieckmann缩合，水解脱羧和与Grignard试剂反应合成了12个均未见文献报道的目标化合物6a─6l，结构均经过1H NMR、IR、MS及元素分析确证。并采用MTT法对目标化合物进行了对白血病K562细胞系增殖影响的初步测试，结果表明大部分具有较好的抑制细胞系增殖的活性，有潜在的抗白血病活性。
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| 关 键 词： | 哌啶衍生物；合成；抑制；K562；MTT |
| 收稿时间： | 2008-04-25 |
| 修稿时间： | 2008-09-25 |
Synthesis and Preliminary Anti‐leukemia Activity of N‐(Substituted Benzyl)‐4‐hydroxy‐4‐substituted Piperidine Derivatives |
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| Zhikun FANG,Sijia XUE,Long CHEN,Yang XU,Anqin YIN,Chunyan LI. Synthesis and Preliminary Anti‐leukemia Activity of N‐(Substituted Benzyl)‐4‐hydroxy‐4‐substituted Piperidine Derivatives[J]. Chinese Journal of Chemistry, 2009, 27(2): 397-402. DOI: 10.1002/cjoc.200990065 |
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| Authors: | Zhikun FANG Sijia XUE Long CHEN Yang XU Anqin YIN Chunyan LI |
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| Affiliation: | 1. Department of Chemistry, College of Life and Environmental Science, Shanghai Normal University, Shanghai 200234, China;2. Tel.: 0086‐021‐64321926;3. Fax: 0086‐021‐64321926 |
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| Abstract: | In order to find some lead compounds with high inhibition against leukemia, twelve unreported compounds 6a – 6l have been synthesized with substituted benzylamines as raw materials via a series of Michael addition, Dieckmann condensation, hydrolysis decarboxylation and reactions with Grignard reagent. Complete assignments have been achieved for the title compounds by 1H NMR, IR, MS and elemental analysis. The preliminary anti‐tumor activity tests indicate that the title compounds have good effect on the cellular growth inhibition against K562 cells and have potential anti‐leukemia bioactivity. |
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| Keywords: | piperidine derivative synthesis inhibition K562 MTT |
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