| 2,5-二酮哌嗪衍生物的一锅法合成及其细胞毒活性 |
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| 引用本文： | 李晋昇,廖升荣,汤勇,刘永宏.2,5-二酮哌嗪衍生物的一锅法合成及其细胞毒活性[J].合成化学,2015,23(12):1095-1099. |
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| 作者姓名： | 李晋昇 廖升荣 汤勇 刘永宏 |
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| 作者单位： | 1. 中国科学院 南海海洋研究所，广东 广州 510301； 2. 中国科学院大学，北京 100049 |
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| 基金项目： | 国家自然科学基金青年基金资助项目（21402218） |
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| 摘 要： | 以DMF为溶剂，Cs2CO3为碱， N,N-二乙酰基-2,5-二酮哌嗪，芳醛和卤代烷经一锅法合成了１10个2,5-二酮哌嗪类衍生物（4a~4j，其中4c, 4f和4i为新化合物），收率54.2％～75.7％，其结构经1H NMR， 13C NMR和ESI-MS确证。生物活性研究结果表明：（Z）-1-乙酰基-3-（1-亚甲基萘）-4-烯丙基-2,5-二酮哌嗪（4c）对U937, Hela和Du145等细胞具有一定的细胞毒活性。
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| 关 键 词： | 2 5-二酮哌嗪 一锅法 Aldol缩合 合成 细胞毒活性 |
| 收稿时间： | 2015-01-16 |
Synthesis and Cytotoxic Activities of 2,5-Diketopiperazine Derivatives by One-pot Method |
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| LI Jin-sheng,LIAO Sheng-rong,TANG Yong,LIU Yong-hong.Synthesis and Cytotoxic Activities of 2,5-Diketopiperazine Derivatives by One-pot Method[J].Chinese Journal of Synthetic Chemistry,2015,23(12):1095-1099. |
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| Authors: | LI Jin-sheng LIAO Sheng-rong TANG Yong LIU Yong-hong |
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| Institution: | 1. South China Sea Institute of Oceanology, Chinese Academy of Sciences, Guangzhou 510301, China; 2. University of Chinese Academy of Sciences, Beijing 100049, China |
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| Abstract: | Ten 2,5-diketopiperazine derivatives(4a~4j, 4c, 4f and 4i were novel compounds) in yield of 54.2～75.7％ were synthesized by Aldol reaction of N,N-diacetyl-2,5-diketopiperazine, arylaldehyde and RX by one pot method, using DMF as the solvent and Cs2CO3 as the alkali. The structures were confirmed by 1H NMR， 13C NMR and ESI-MS. Preliminary biological activities tests indicated that (Z)-1-acetyl-4-allyl-3-(naphthalen-1-ylmethylene)piperazine-2,5-dione(4c) exhibited better cytotoxic activities against U937, Hela and Du145 cell lines. |
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| Keywords: | 2 5-diketopiperazine one-pot method Aldol condensation synthesis cytotoxic activity |
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