华东理工大学学报（自然科学版）2017，Vol.43Issue(1)：1-7,15,8.DOI:10.14135/j.cnki.1006-3080.2017.01.001
一种新型开环烯二炔的设计、合成及细胞毒性研究
Design,Synthesis and Cytotoxicity Study of a Novel Acyclic Enediyne
摘要
Abstract
An acyclic enediyne with maleimide as the main structure and two symmetrical alkynyl chains was synthesized through Sonogashira coupling reaction.The enediyne was subj ected to thermal Bergman cyclization to yield diradical intermediates.FT-IR results showed the complete conversion of the alkynyl moiety.The diradical intermediates could be further trapped by a spin trap (PBN)to generate mono-and di-PBN adducts corroborating the occurrence of the Bergman cyclization,which was confirmed by EPR analysis.MTT cell activity experiments confirmed that the half inhibitory concentration of this small molecular enediyne on tumor cell was around 18μmol/L which were stable enough for long-time storage and active enough to suppress the cell multiplication for potential clinical application.关键词
烯二炔/Bergman环化/抗肿瘤抗生素/细胞毒性Key words
enediyne/Bergman cyclization/antibiotics/cytotoxicity分类
化学化工引用本文复制引用
黄帅,李竞,李保君,胡爱国..一种新型开环烯二炔的设计、合成及细胞毒性研究[J].华东理工大学学报（自然科学版）,2017,43(1):1-7,15,8.基金项目
国家自然科学基金项目(21474027) （21474027）
