文献类型：期刊文献

英文题名：Selenium-containing naphthalimides as anticancer agents: Design, synthesis and bioactivity

作者：Zhao, Liwei[1,2];Li, Jianfeng[1];Li, Yiquan[1];Liu, Jianwen[1];Wirth, Thomas[2];Li, Zhong[1]

机构：[1]E China Univ Sci & Technol, Sch Pharm, Shanghai Key Lab Chem Biol, Shanghai 200237, Peoples R China;[2]Cardiff Univ, Sch Chem, Cardiff CF10 3AT, S Glam, Wales

年份：2012

卷号：20

期号：8

起止页码：2558

外文期刊名：BIOORGANIC & MEDICINAL CHEMISTRY

收录：;WOS:【SCI-EXPANDED(收录号:WOS:000302767100009)】；

基金：This work was financially supported by the National Basic Research Program of China (973 Program, 2010CB126100), National High Technology Research, the Development Program of China (863 Program, 2011AA10A207), and the National Key Technology R&D Program of China (2011BAE06B01). This work was also partly supported by the Fundamental Research Funds for the Central Universities. The authors would like to thank Professors Jianwen Liu and Yiquan Li from School of Pharmacy, East China University and Science and Technology, for anticancer evaluation and valuable suggestions.

语种：英文

外文关键词：Anticancer; Naphthalimides; Selenium; K562; DNA

摘要：Selenium analogues (4b-4h, and 4j) of two known sulfur compounds were synthesized and tested their anticancer activities. The selenium compound 4b had comparable activity with its sulfur analogue 4a, while DNA-binding study showed these two compounds had similar interaction with ct-DNA, the K-b was 8.23 and 2.36, respectively. The primary results showed that most compounds had moderate anticancer activities with IC50 values between 10 (6) and 10 (5) M. Another selenium analogue 4j showed the highest activity with the IC50 values around 5.3 mu M against K562 and MCF-7 cell lines. More importantly, the organochalcogen compounds exhibited stronger anticancer activities against K562 cell line than the other cell lines tested. Crown Copyright (C) 2012 Published by Elsevier Ltd. All rights reserved.