烟台大学学报(自然科学与工程版)2017,Vol.30Issue(4):301-306,334,7.DOI:10.13951/j.cnki.37-1213/n.2017.04.006
5,6-二取代苯并氧化呋咱类似物的合成与体外抗肿瘤活性研究
Synthesis and Antitumor Activities in vitro of 5,6-Disubstituted Benzofuroxan Analogues
摘要
Abstract
Fifteen 5,6-disubstituted benzofuroxan analogues are synthesized from 2,4-dichloro-nitrobenzene by the reactions of nitration,amino substitution,azidation and cyclization.Their structures are characterized by 1H NMR and HRMS.Their antitumor activities in vitro against NCI H460,MCF-7 and HCT-116 are evaluated by SRB assay.In the preliminary study,it is found that most of the target compounds (5 μmol/L) show certain extent of inhibition against cancer cells.The inhibition rates of 4k、41 and 4o against colon cancer HCT-116 cells are above 60%;the inhibition rates of 4a,4d,4k,41 and 4o against breast cancer MCF-7 cells are above 85%.The IC50 of 4o against breast cancer MCF-7 cells is 1.6 μmol/L.关键词
苯并氧化呋咱/衍生物/合成/体外抗肿瘤活性Key words
benzofuroxan/derivatives/synthesis/antitumor activity in vitro分类
医药卫生引用本文复制引用
徐阳荣,赵风兰,谭文娟,安行思,刘智,孟庆国,杜广营..5,6-二取代苯并氧化呋咱类似物的合成与体外抗肿瘤活性研究[J].烟台大学学报(自然科学与工程版),2017,30(4):301-306,334,7.基金项目
烟台大学2016年研究生科技创新基金项目(YDYB1627). (YDYB1627)