| 毛泽伟,万春平,张梦迪,郑 喜,饶高雄.化学通报,2016,79(4):381-383. |
| 氮杂岩白菜素衍生物的合成及其初步抗肿瘤活性 |
| Synthesis and preliminary anti-tumor activity of Aza-Bergenin derivatives |
| 投稿时间：2015-09-01 修订日期：2015-10-22 |
| DOI： |
| 中文关键词: 岩白菜素 衍生物 合成 抗肿瘤活性 |
| 英文关键词:Bergenin, derivatives, synthesis, anti-tumor activity |
| 基金项目:云南省应用基础研究计划项目 |
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| 中文摘要: |
| Bergenin is attracting more attention having a wide range of biological activities. In this work, eight Aza-Bergenin derivatives were synthesized by the Mannich reaction and Mitsunobu reaction, the structures were characterized by 1H-NMR, 13C-NMR and HRMS. Their anti-tumor activities were studied in vitro against human tumor cell line A549 by the MTT assay. The result revealed that compound 3c and 3d were found to be the most potent compounds against A549（IC50=3.74μM and 5.05μM, respectively）, which showed better activity than Bergenin and to be lead compounds for further research. |
| 英文摘要: |
| Bergenin is attracting more attention having a wide range of biological activities. In this work, eight Aza-Bergenin derivatives were synthesized by the Mannich reaction and Mitsunobu reaction, the structures were characterized by 1H-NMR and 13C-NMR. Their anti-tumor activities were studied in vitro against human tumor cell line A549 by the MTT assay. The result revealed that compound 3c（IC50=3.74μM）and 3d（IC50=5.05μM）were found to be the most potent compounds against A549, which are more active than Bergenin and to be lead compounds for further research. |
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