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题名: Novel angular furoquinolinones bearing flexible chain as antitumor agent: Design, synthesis, cytotoxic evaluation, and DNA-binding studies
作者: Xie, Lijuan1;  Qian, Xuhong1, 2;  Cui, Jingnan1;  Xiao, Yi1;  Wang, Kewei1;  Wu, Peichun3;  Cong, Liying1
关键词: DNA-intercalator ;  antitumor ;  furoquinolinone ;  N-substituted furoquinolinone
刊名: BIOORGANIC & MEDICINAL CHEMISTRY
发表日期: 2008-09-15
DOI: 10.1016/j.bmc.2008.07.081
卷: 16, 期:18, 页:8713-8718
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology ;  Life Sciences & Biomedicine ;  Physical Sciences
类目[WOS]: Biochemistry & Molecular Biology ;  Chemistry, Medicinal ;  Chemistry, Organic
研究领域[WOS]: Biochemistry & Molecular Biology ;  Pharmacology & Pharmacy ;  Chemistry
英文摘要: 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.
关键词[WOS]: BETA-CARBOLINE DERIVATIVES ;  BIOLOGICAL EVALUATION ;  CANCER-THERAPY ;  SIDE-CHAINS ;  MODE ;  INTERCALATORS ;  MOLECULES ;  MECHANISM ;  EFFICIENT ;  PSORALEN
语种: 英语
WOS记录号: WOS:000259173400045
Citation statistics: 
内容类型: 期刊论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/141034
Appears in Collections:中国科学院大连化学物理研究所_期刊论文

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作者单位: 1.Dalian Univ Technol, State Key Lab Fine Chem, Dalian 116012, Peoples R China
2.E China Univ Sci & Technol, Sch Pharm, Shanghai Key Lab Chem Biol, Shanghai 200237, Peoples R China
3.Chinese Acad Sci, Dalian Inst Chem Phys, Marine Bioprod Engn Grp, Dalian 116023, Peoples R China

Recommended Citation:
Xie, Lijuan,Qian, Xuhong,Cui, Jingnan,et al. Novel angular furoquinolinones bearing flexible chain as antitumor agent: Design, synthesis, cytotoxic evaluation, and DNA-binding studies[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2008,16(18):8713-8718.
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