个人信息Personal Information
教授
硕士生导师
性别:女
毕业院校:大连理工大学
学位:博士
所在单位:化工学院
学科:应用化学. 精细化工. 有机化学
办公地点:化工实验楼E座514
联系方式:0411-84986324 13504280675
电子邮箱:xlianli@dlut.edu.cn
Novel DNA intercalators without basic side chains as efficient antitumor agents: Design, synthesis and evaluation of benzo-[c,d]-indol-malononitrile derivatives
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论文类型:期刊论文
发表时间:2010-05-01
发表刊物:BIOORGANIC & MEDICINAL CHEMISTRY
收录刊物:SCIE、PubMed、Scopus
卷号:18
期号:9
页面范围:3279-3284
ISSN号:0968-0896
关键字:Benzo[c,d]indol-2(1H)-one; Antitumor agents; DNA intercalator; DNA cleavage
摘要:Several 2-(substituted benzo[c,d]indol-2(1H)-ylidene) malononitriles have been designed and synthesized. Their DNA binding, antitumor and DNA damaging properties were evaluated. All the compounds exhibited efficient antitumor activities with preference to be against the tumor cell line 7721 rather than the tumor cell line MCF-7. Compound 1f could intercalate into DNA entirely presumably by the good conjugation of carbonyl group with benzo[c,d] indol moiety. What's more, 1f exhibited potent toxicity against MCF-7 cells with IC(50) at 0.003 mu M and against 7721 cells at 0.115 mu M, respectively. (C) 2010 Elsevier Ltd. All rights reserved.