Document Detail

Synthesis and antiproliferative evaluation of 4-anilino-n-methoxyfuro[2,3-b]quinoline derivatives (n=6, 7). Part 5.
MedLine Citation:
PMID:  18293440     Owner:  NLM     Status:  MEDLINE    
A series of 27 differently substituted 4-anilinofuro[2,3-b]quinolines were synthesized and evaluated for their antiproliferative activities against the HeLa, SKHep1, SAS, AGS, A549, and CE81T cell lines, cancers commonly found in Asian countries. Among the compounds tested, 1-{4-[(3-chloro-7-methoxyfuro[2,3-b]quinolin-4-yl)amino]phenyl}ethanone (1) was the most potent, with IC(50) values of 3.1, 3.0, and 4.2 microM, resp., against the growth of HeLa, SKHep, and CE81T cells. Compound 1 was, thus, further evaluated by flow cytometry to evaluate its effect on the cell-cycle distribution of HeLa cells. Our results indicated that 1 readily induces cell-cycle arrest in the G2/M phase, followed by DNA fragmentation and, ultimately, cell death.
Yeh-Long Chen; Huan-Chin Lin; Chia-Ning Yang; Pei-Jung Lu; Cherng-Chyi Tzeng
Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Chemistry & biodiversity     Volume:  5     ISSN:  1612-1880     ISO Abbreviation:  Chem. Biodivers.     Publication Date:  2008 Feb 
Date Detail:
Created Date:  2008-02-28     Completed Date:  2008-10-17     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  101197449     Medline TA:  Chem Biodivers     Country:  Switzerland    
Other Details:
Languages:  eng     Pagination:  267-78     Citation Subset:  IM    
Faculty of Medicinal and Applied Chemistry, College of Life Science, Kaohsiung Medical University, Kaohsiung City 807, Taiwan.
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MeSH Terms
Aniline Compounds / chemical synthesis*,  chemistry,  pharmacology*
Antineoplastic Agents, Phytogenic / chemical synthesis*,  chemistry,  pharmacology*
Cell Line, Tumor
Cell Proliferation / drug effects
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Flow Cytometry / methods
Hela Cells
Inhibitory Concentration 50
Magnetic Resonance Spectroscopy / methods,  standards
Molecular Conformation
Quinolines / chemical synthesis*,  chemistry,  pharmacology*
Reference Standards
Structure-Activity Relationship
Reg. No./Substance:
0/4-anilino-n-methoxyfuro(2,3-b)quinoline; 0/Aniline Compounds; 0/Antineoplastic Agents, Phytogenic; 0/Quinolines

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