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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  ;  Youngjoo Kwon  ;  Younghwa Na  ;  Hea-Young Park Choo  ;  Eung-Seok Lee  ;  Ok-Hee Lee  ;  Mi-Ja Jung 
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
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
https://ir.ymlib.yonsei.ac.kr/handle/22282913/94042
DOI
10.1016/j.ejmech.2011.01.011
Appears in Collections:
1. Journal Papers (연구논문) > 5. Research Institutes (연구소) > Yonsei Integrative Research Institute for Cerebral & Cardiovascular Disease (뇌심혈관질환융합연구사업단)
Yonsei Authors
이옥희(Lee, Ok Hee)
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Full Text
http://www.sciencedirect.com/science/article/pii/S0223523411000195
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