文献类型：期刊文献

英文题名：Maleimide-based acyclic enediyne for efficient DNA-cleavage and tumor cell suppression

作者：Song, Depeng[1];Sun, Shiyuan[1];Tian, Yu[2];Huang, Shuai[1];Ding, Yun[3];Yuan, Yuan[2];Hu, Aiguo[1]

机构：[1]E China Univ Sci & Technol, Sch Mat Sci & Engn, Shanghai Key Lab Adv Polymer Mat, Shanghai 200237, Peoples R China;[2]E China Univ Sci & Technol, State Key Lab Bioreactor Engn, Shanghai 200237, Peoples R China;[3]Univ Svizzera Italiana, Dept Chem & Appl Biosci, Eidgenossische Tech Hsch Zurich & Facolta Informa, Inst Sci Computat, CH-6900 Lugano, Switzerland

年份：2015

卷号：3

期号：16

起止页码：3195

外文期刊名：JOURNAL OF MATERIALS CHEMISTRY B

收录：;EI(收录号：20151700773063);WOS:【SCI-EXPANDED(收录号:WOS:000352867800009)】；

基金：The authors acknowledge the financial support from National Natural Science Foundation of China (21274042, 21474027) and the Shanghai Leading Academic Discipline Project (B502). A.H. thanks the "Eastern Scholar Professorship" support from Shanghai local government. D.S. thanks Dr Liujing Wei and Prof. Qiang Hua for their support and helpful discussions on electrophoresis and Prof. Linyong Zhu for his help in UV-vis analysis.

语种：英文

外文关键词：Tumors - Cyclization - Cytology - Cells - DNA

摘要：A pH-sensitive acyclic enediyne (1) was synthesized for efficient DNA-cleavage and tumor cell suppression. Unlike other acyclic enediynes, this novel enediyne transforms into a highly reactive enediyne (2) in an acidic environment only, which undergoes Bergman cyclization spontaneously at ambient temperature. An EPR study on the enediyne 2 confirmed the generation of free radicals through Bergman cyclization. The activated enediyne induced DNA-cleavage and exhibited cytotoxicity towards various tumor cells under the action of diradicals arising from spontaneous Bergman cyclization at physiological temperature. These findings suggest a novel strategy of anticancer drug design, where the activation of the silent compound takes place under the acidic environment inside the tumor cells.