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Synthesis, biological evaluation, and molecular docking study of 3-(3'-heteroatom substituted-2'-hydroxy-1'-propyloxy) xanthone analogues as novel topoisomerase IIα catalytic inhibitor.

Authors
 Kyu-Yeon Jun  ;  Eun-Young Lee  ;  Mi-Ja Jung  ;  Ok-Hee Lee  ;  Eung-Seok Lee  ;  Hea-Young Park Choo  ;  Younghwa Na  ;  Youngjoo Kwon 
Citation
 EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, Vol.46(6) : 1964-1971, 2011 
Journal Title
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
ISSN
 0223-5234 
Issue Date
2011
MeSH
Antigens, Neoplasm/metabolism ; Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Antineoplastic Agents/pharmacology* ; Biocatalysis/drug effects ; Cell Line, Tumor ; Cell Survival/drug effects ; DNA Topoisomerases, Type II/metabolism ; DNA-Binding Proteins/antagonists & inhibitors* ; DNA-Binding Proteins/metabolism ; Dose-Response Relationship, Drug ; Drug Screening Assays, Antitumor ; HL-60 Cells ; HeLa Cells ; Humans ; Models, Molecular ; Molecular Structure ; Stereoisomerism ; Structure-Activity Relationship ; Topoisomerase II Inhibitors/chemical synthesis ; Topoisomerase II Inhibitors/chemistry ; Topoisomerase II Inhibitors/pharmacology* ; Xanthones/chemical synthesis ; Xanthones/chemistry ; Xanthones/pharmacology*
Keywords
Xanthones ; Anti-cancer agents ; ATP-competitive topoisomerase IIα inhibitor ; Molecular docking
Abstract
Epoxide ring-opened xanthone derivatives were synthesized and tested for their topoisomerase inhibitory activity and cytotoxicity. Most of the compounds showed topo IIα specific inhibitory activity. To clarify the mechanism of action of these compounds, the most potent compound (compound 14) of the synthesized analogues was further studied by testing its ATPase inhibitory activity and through molecular docking experiments. The results showed that the topo IIα inhibitory activity of compound 14 was inversely proportional to ATP concentration. In the ATPase inhibitory test, ATP hydrolysis was reduced less efficiently by compound 14 (28.5±4.6%) than novobiocin (60.4±8.1%). Molecular docking study revealed compound 14 to have a stable binding pattern to the ATP-binding domain of human topo II.
Full Text
http://www.sciencedirect.com/science/article/pii/S0223523411000195
DOI
10.1016/j.ejmech.2011.01.011
Appears in Collections:
1. College of Medicine (의과대학) > Research Institute (부설연구소) > 1. Journal Papers
Yonsei Authors
Lee, Ok Hee(이옥희)
URI
https://ir.ymlib.yonsei.ac.kr/handle/22282913/94042
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