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个人信息Personal Information
教授
博士生导师
硕士生导师
性别：男
毕业院校：日本冈山大学
学位：博士
所在单位：化工学院
学科：精细化工. 应用化学
办公地点：大连理工大学西部校区E209
联系方式：13591789942
电子邮箱：jncui@dlut.edu.cn
Novel angular furoquinolinones bearing flexible chain as antitumor agent: Design, synthesis, cytotoxic evaluation, and DNA-binding studies
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论文类型：期刊论文
发表时间：2008-09-15
发表刊物：BIOORGANIC & MEDICINAL CHEMISTRY
收录刊物：SCIE、PubMed、Scopus
卷号：16
期号：18
页面范围：8713-8718
ISSN号：0968-0896
关键字：DNA-intercalator; antitumor; furoquinolinone; N-substituted furoquinolinone
摘要：A series of novel N-substituted angular furoquinolinone derivatives were synthesized and evaluated for their antitumor activities against QGY, K562, HeLa, P388, and A549 cell lines in vitro. The derivatives bearing basic amino side chain showed an improved antitumor activity. Compound 5h N-(2-dimethylaminoethyl)-2-(4,8,9-trimethyl-2-oxo-2H-furo[2,3-h]quinolin-1-yl)-acetamide exhibited the highest activities against P388 and A549 cell lines, which are evidenced by the IC(50) values that are four to five fold lower than that for unsubstituted parent compound. DNA-binding experiments suggested that these derivatives bind to DNA through intercalation. (C) 2008 Elsevier Ltd. All rights reserved.