| N-呋喃酮基磺酰肼的合成与抗肿瘤活性研究 |
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| 引用本文： | 吴桂贞,陈任宏,杨凯,刘海,汪朝阳.N-呋喃酮基磺酰肼的合成与抗肿瘤活性研究[J].化学研究与应用,2020,32(6):1053-1059. |
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| 作者姓名： | 吴桂贞 陈任宏 杨凯 刘海 汪朝阳 |
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| 作者单位： | 广东食品药品职业学院,广东 广州 510520;华南师范大学化学学院,广东 广州 510006;赣南医学院药学院,江西 赣州 341000;赣南医学院药学院,江西 赣州 341000;华南师范大学化学学院,广东 广州 510006 |
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| 基金项目： | 广东食品药品职业学院自然科学研究项目;广东省自然科学基金;广东省医学科学技术研究项目;国家自然科学基金 |
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| 摘 要： | 以5-甲氧基-3,4-二卤-2(5H)-呋喃酮和磺酰肼为原料,DMAP为催化剂,设计合成10个N-呋喃酮基磺酰肼类化合物(4a^4j),产率在75~92%之间,并通过1H NMR对所有目标化合物进行了结构表征。采用MTT法测定目标化合物对人乳腺癌(MCF-7)、人神经胶质瘤(U87)、人肺癌(A549)细胞的体外抑制活性,结果显示部分目标化合物表现出较好的抗肿瘤活性,其中化合物4d效果最佳,对MCF-7、U87、A549的IC50值分别达到7.33±0.36μmol·L^-1、5.68±0.28μmol·L^-1和17.09±0.23μmol·L^-1。
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| 关 键 词： | 2(5H)-呋喃酮 磺酰肼 DMAP 抗肿瘤活性 |
Synthesis and anti-tumor activities of N-furanonyl arylsulfonyl hydrazides derivatives |
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| WU Gui-zhen,CHEN Ren-hong,YANG Kai,LIU Hai,WANG Zhao-yang.Synthesis and anti-tumor activities of N-furanonyl arylsulfonyl hydrazides derivatives[J].Chemical Research and Application,2020,32(6):1053-1059. |
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| Authors: | WU Gui-zhen CHEN Ren-hong YANG Kai LIU Hai WANG Zhao-yang |
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| Institution: | (Guangdong Food and Drug Vocational College,Guangzhou 510520,China;School of Chemistry and Environment,South China Normal University,Guangzhou 510006,China;School of Pharmacy,Gannan Medical University,Ganzhou 341000,China) |
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| Abstract: | Using DMAP as catalyst,5-methoxy-3,4-dihalo-2(5H)-furanone and sulfonyl hydrazides as start materials,ten N-furanonyl arylsulfonyl hydrazides(4a^4j)were synthesized.The yields were between 75%and 92%.And the chemical structure of target compounds were characterized by 1H NMR.What’s more,the test of inhibitory activities in vitro by MTT with human breast cancer cells(MCF-7),glioma cells(U87)and lung cancer cells(A549)showed that parts of these compounds had good anti-tumor activities.Among them,the inhibitory activity of compound 4d was the best,and its proliferation inhibition was 7.33±0.36μmol·L^-1 for MCF-7,5.68±0.28μmol·L^-1 for U87 and 17.09±0.23μmol·L^-1 for A549,respectively. |
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| Keywords: | 2(5H)-furanone sulfonylhydrazide DMAP anti-tumor activity |
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