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New insight for fluoroquinophenoxazine derivatives as possibly new potent topoisomerase I inhibitor

Title
New insight for fluoroquinophenoxazine derivatives as possibly new potent topoisomerase I inhibitor
Authors
Kang D.-H.Kim J.-S.Jung M.-J.Lee E.-S.Jahng Y.Kwon Y.Na Y.
Ewha Authors
권영주
SCOPUS Author ID
권영주scopus
Issue Date
2008
Journal Title
Bioorganic and Medicinal Chemistry Letters
ISSN
0960-894XJCR Link
Citation
vol. 18, no. 4, pp. 1520 - 1524
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
Fluoroquinolones, represented by ciproxacin and norfloxacin, are well-known clinical antimicrobial agents, and their phenyl ring expanded quinophenoxazines are reported as possible antitumor active compounds. These quinophenoxazines are known to inhibit DNA topoisomerase II essential for cell replication cycle. But there were no reports for topoisomerase I inhibition study for these compounds. In this report, we have prepared a few quinophenoxazine analogues and tested their topoisomerases I and II inhibitory activities and cytotoxicity. From the result, we found that quinophenoxazine analogues possessed strong topoisomerase I inhibitory capacity as well as topoisomerase II inhibition. Among the compounds prepared, A-62176 analogues showed strong topoisomerases I and II inhibitory activities. Interestingly, compound 8 missing the 3-aminopyrrolidine moiety at C2 position has similar potent inhibitory capacity against topoisomerases I and II at higher concentrations (20 and 10 μM, respectively). But compound 8 inhibited topoisomerase I function more selectively at lower concentration, 2 μM. Our observation might strongly implicate that fluoroquinophenoxazines can be developed as efficient topoisomerase I inhibitor with the elaborate modification. © 2007 Elsevier Ltd. All rights reserved.
DOI
10.1016/j.bmcl.2007.12.053
Appears in Collections:
약학대학 > 약학과 > Journal papers
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