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Molecular design, synthesis and docking study of benz[b]oxepines and 12-oxobenzo[c]phenanthridinones as topoisomerase 1 inhibitors

Title
Molecular design, synthesis and docking study of benz[b]oxepines and 12-oxobenzo[c]phenanthridinones as topoisomerase 1 inhibitors
Authors
Lee S.-H.Van H.T.M.Yang S.H.Lee K.-T.Kwon Y.Cho W.-J.
Ewha Authors
권영주
SCOPUS Author ID
권영주scopus
Issue Date
2009
Journal Title
Bioorganic and Medicinal Chemistry Letters
ISSN
0960-894XJCR Link
Citation
vol. 19, no. 9, pp. 2444 - 2447
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
Benz[b]oxepines 4a-g and 12-oxobenzo[c]phenanthridines 5a-d were designed and synthesized as constrained forms of 3-arylisoquinolines through an intramolecular radical cyclization reaction. Radical cyclization of O-vinyl compounds preferentially led to the 7-endo-trig cyclization pathway to the benz[b]oxepines and 12-oxobenzo[c]phenanthridines through 6-exo-trig path as minor products. Among the synthesized compounds, benz[b]oxepine derivative 4e exhibited potent in vitro cytotoxicity against three different tumor cell lines, as well as topoisomerase 1 inhibitory activity. A Surflex-Dock docking study was performed to clarify the topoisomerase 1 activity of 4e. © 2009 Elsevier Ltd. All rights reserved.
DOI
10.1016/j.bmcl.2009.03.058
Appears in Collections:
약학대학 > 약학과 > Journal papers
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