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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.