| 刘志平,甘春芳,黄燕敏,崔建国,韦万兴.化学通报,2021,84(1):90-95. |
| 多肟基柚皮素衍生物的合成与细胞毒活性 |
| Syntheses and Cytotoxicities of Polyoxime Naringin Derivatives |
| 投稿时间：2020-07-14 修订日期：2020-09-05 |
| DOI： |
| 中文关键词: 柚皮素 多肟基 细胞毒活性 |
| 英文关键词:Naringin Polyoxime Cytotoxicity |
| 基金项目:广西自然科学基金项目（2019JJA120062）和南宁师范大学博士启动基金项目（602021239052）资助 |
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| 中文摘要: |
| 以天然产物柚皮素（1）为原料，分别与α-溴代苯乙酮、α-溴代-4-氯苯乙酮、1-（2-溴乙基）-3-吲哚甲醛、α-溴代丙酮进行醚化反应得到7-（2-氧代-2-苯基乙氧基）柚皮素、7-（2-氧代-2-（4-氯苯基）乙氧基）柚皮素、7-（2-（3-甲酰基吲哚）乙氧基）柚皮素、7，4'-二（2-氧代丙氧基）柚皮素，然后分别与盐酸羟胺、盐酸甲氧胺进行肟化反应，合成了8种多肟基柚皮素衍生物6~13，并通过红外光谱、核磁共振谱及高分辨质谱进行了结构表征。噻唑蓝（MTT）蛋白染色法体外抑制肿瘤增值活性测试显示化合物10、12对人胃癌细胞SGC-7901有较好的抑制活性，其IC50值分别为16.4和15.3 μmol/L。 |
| 英文摘要: |
| Taking natural product naringenin as raw material, it was etherified with α-bromoacetophenone, 4-chloro-α-bromoacetophenone, 1-(2-bromoethyl)-indole-3-formaldehyde and α-bromoacetone respectively. Then the intermediate products were subjected to oximation reaction with hydroxylamine hydrochloride and methoxyamine hydrochloride to obtained eight polyoxime naringin derivatives 6~13. Their structures were determined by IR, NMR and HR-MS. The cytotoxic activities of the target compounds were evaluated against SGC-7901 by MTT method in vitro. The results showed that the compounds 10 and 12 display distinct antiproliferative activity against SGC-7901 with the values of IC50 16.4 and 15.3 μmol/L, respectively. |
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