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.
作者
吴桂贞
陈任宏
杨凯
刘海
汪朝阳
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)
出处
《化学研究与应用》
CAS
CSCD
北大核心
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。
