Design, synthesis and biological evaluation of E-ring modified evodiamine derivatives as novel antitumor agents

作     者：Kun Fang Guo-Qiang Dong Hai Gong Na Liu Zhen-Gang Li Shi-Ping Zhu Zhen-Yuan Miao Jian-Zhong Yao Wan-Nian Zhang Chun-Quan Sheng 

作者机构：School of Pharmacy Second Military Medical University Department of Radiation OncologyJi’nan Military General Hospital 

基　　金：supported by National Natural Science Foundation of China(Nos.81222044,81373278) Key Project of Science and Technology of Shanghai(No.11431920402) the National Basic Research Program of China(No.2014CB541800) Shanghai Rising Star Program(No.12QH1402600) Shanghai Municipal Health Bureau(No.XYQ2011038) 

出 版 物：《Chinese Chemical Letters》 (中国化学快报（英文版）)

年 卷 期：2014年第25卷第7期

页      码：978-982页

摘      要：A series of novel E-ring modified evodiamine derivatives were designed and synthesized as antitumor agents. Their capacity to interfere with the catalytic activity of topoisomerase Ⅰ and Ⅱ was evaluated by the relaxation assay. In vitro antitumor activity results revealed that compound 12 showed good antitumor activity with a broad spectrum. Its binding modes with topoisomerase Ⅰ and Ⅱ were clarified by molecular docking.

主 题 词：Evodiamine derivatives Topoisomerase Ⅰ Topoisomerase Ⅱ Antitumor activity 

学科分类：090403[090403] 09[农学] 0904[农学-动物医学类] 

核心收录：

D　O　I：10.1016/j.cclet.2014.03.043

馆 藏 号：203115360...