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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.

Title
 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 ; Youngjoo Kwon ; Younghwa Na ; Hea-Young Park Choo ; Eung-Seok Lee ; Ok-Hee Lee ; Mi-Ja Jung 
Issue Date
2011
Journal Title
 European Journal of Medicinal Chemistry 
ISSN
 0223-5234 
Citation
 European Journal of Medicinal Chemistry, Vol.46(6) : 1964~1971, 2011 
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.
URI
http://ir.ymlib.yonsei.ac.kr/handle/22282913/94042
DOI
10.1016/j.ejmech.2011.01.011
Appears in Collections:
1. 연구논문 > 5. Research Institutes > Yonsei Integrative Research Institute for Cerebral & Cardiovascular Disease
Yonsei Authors
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Link
 http://www.sciencedirect.com/science/article/pii/S0223523411000195
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