Document Detail


Synthesis of 2-styrylchromones as a novel class of antiproliferative agents targeting carcinoma cells.
MedLine Citation:
PMID:  19246129     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
A series of 2-styrylchromone analogs were synthesized and examined for their antiproliferative effects on a panel of carcinoma cells. Among the tested agents, only 4m exhibited a moderate activity with an IC(50) value of 28.9 microM against PC-3 cells which indicates the selectivity of PC-3 cells in response to 2-styrylchromones. In addition, 4q demonstrated the most antiproliferative effect with an IC(50) value of 4.9 microM against HeLa cells. Flow cytometric analysis and DAPI staining revealed that HeLa cells exposed to 4q as low as 5 microM induced cell death through sub-G1 arrest and DNA fragmentation. Furthermore, CoMFA analysis of tested 2-styrylchromones resulted in a q(2) of 0.459 to generate a 3D-QSAR model on BT483 cell line. Together, these results suggest a potential structural optimization and pharmacological study of 2-styrylchromones.
Authors:
Arthur Y Shaw; Chun-Yi Chang; Hao-Han Liau; Pei-Jung Lu; Hui-Ling Chen; Chia-Ning Yang; Hao-Yi Li
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2009-02-06
Journal Detail:
Title:  European journal of medicinal chemistry     Volume:  44     ISSN:  1768-3254     ISO Abbreviation:  Eur J Med Chem     Publication Date:  2009 Jun 
Date Detail:
Created Date:  2009-04-20     Completed Date:  2009-07-15     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0420510     Medline TA:  Eur J Med Chem     Country:  France    
Other Details:
Languages:  eng     Pagination:  2552-62     Citation Subset:  IM    
Affiliation:
Department of Chemistry, Tamkang University, Tamsui 251, Taiwan. shaw299@mail.tku.edu.tw
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MeSH Terms
Descriptor/Qualifier:
Apoptosis / drug effects
Cell Cycle / drug effects
Cell Line, Tumor
Cell Proliferation / drug effects
Cell Survival / drug effects
Chromones / chemical synthesis*,  classification,  pharmacology*
Dose-Response Relationship, Drug
Drug Design*
Drug Screening Assays, Antitumor
Fluorescent Antibody Technique
Hela Cells
Humans
Male
Models, Molecular
Molecular Structure
Prostatic Neoplasms / drug therapy*,  pathology
Quantitative Structure-Activity Relationship
Stereoisomerism
Styrenes / chemical synthesis*,  classification,  pharmacology*
Time Factors
Chemical
Reg. No./Substance:
0/Chromones; 0/Styrenes

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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