Indexed by:期刊论文

Date of Publication:2008-09-15

Journal:BIOORGANIC & MEDICINAL CHEMISTRY

Included Journals:SCIE、PubMed、Scopus

Volume:16

Issue:18

Page Number:8713-8718

ISSN No.:0968-0896

Key Words:DNA-intercalator; antitumor; furoquinolinone; N-substituted furoquinolinone

Abstract: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.