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

Title
Synthesis, biological evaluation, and molecular docking study of 3-(3 '-heteroatom substituted-2 '-hydroxy-1 '-propyloxy) xanthone analogues as novel topoisomerase II alpha catalytic inhibitor
Author(s)
전규연[전규연]이은영[이은영]정미자[정미자]이옥희[이옥희]이응석박혜영[박혜영]나영화[나영화]권영주[권영주]
Keywords
POTENTIAL ANTICANCER DRUGS; MEDIATED DNA CLEAVAGE; DECATENATION CHECKPOINT; ATPASE DOMAIN; DERIVATIVES; BINDING
Issue Date
201106
Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
Citation
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v.46, no.6, pp.1964 - 1971
Abstract
Epoxide ring-opened xanthone derivatives were synthesized and tested for their topoisomerase inhibitory activity and cytotoxicity. Most of the compounds showed topo II alpha 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 II alpha 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. (C) 2011 Elsevier Masson SAS. All rights reserved.
URI
http://hdl.handle.net/YU.REPOSITORY/25052http://dx.doi.org/10.1016/j.ejmech.2011.01.011
ISSN
0223-5234
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약학대학 > 약학부 > Articles
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