N-呋喃酮基磺酰肼的合成与抗肿瘤活性研究  

Synthesis and anti-tumor activities of N-furanonyl arylsulfonyl hydrazides derivatives

作　　者：吴桂贞[1] 陈任宏[1] 杨凯[2,3] 刘海[3] 汪朝阳[2] WU Gui-zhen;CHEN Ren-hong;YANG Kai;LIU Hai;WANG Zhao-yang(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)

机构地区：[1]广东食品药品职业学院,广东广州510520 [2]华南师范大学化学学院,广东广州510006 [3]赣南医学院药学院,江西赣州341000

出　　处：《化学研究与应用》2020年第6期1053-1059,共7页Chemical Research and Application

基　　金：广东食品药品职业学院自然科学研究项目(2018ZR001)资助;广东省医学科学技术研究基金项目(A2016358)资助;广东省自然科学基金项目(2014A030313429、S2011010001556)资助;国家自然科学基金项目(81860261)资助。

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。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.

关 键 词：2(5H)-呋喃酮 磺酰肼 DMAP 抗肿瘤活性 

分 类 号：O626.1[理学—有机化学]