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Oxiranylmethyloxy or thiiranylmethyloxy-azaxanthones and -acridone analogues as potential topoisomerase I inhibitors

Title
Oxiranylmethyloxy or thiiranylmethyloxy-azaxanthones and -acridone analogues as potential topoisomerase I inhibitors
Authors
Cho H.-J.Jung M.-J.Kwon Y.Na Y.
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. 23, pp. 6766 - 6769
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
A total of seven new oxyranylmethyloxy or thiiranylmethyloxy group substituted 5-azaxanthones and -acridones analogues were synthesized and tested for their biological activities for cancer cell lines and topoisomerases. Among the compounds, compound 5, 3-thiiranylmethyloxy-1-hydroxy-5-azaxanthone, showed effective topoisomerase I inhibitory activity, 50% and 27% inhibition ratio at 100 and 20 μM, respectively. This result is the first finding of the function of 5-azaxanthone compounds for topoisomerase I inhibition and can provide a novel skeleton for the anticancer drug development process. © 2009 Elsevier Ltd. All rights reserved.
DOI
10.1016/j.bmcl.2009.09.091
Appears in Collections:
약학대학 > 약학과 > Journal papers
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