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
作者单位E-mail
刘志平 南宁师范大学化学与材料学院 南宁 530001 liuzhiping828@126.com 
甘春芳 南宁师范大学化学与材料学院 南宁 530001  
黄燕敏 南宁师范大学化学与材料学院 南宁 530001  
崔建国 南宁师范大学化学与材料学院 南宁 530001  
韦万兴 广西大学化学化工学院 南宁 530004  
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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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