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

New insight for fluoroquinophenoxazine derivatives as possibly new potent topoisomerase I inhibitor. Research Abstract Details 

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New insight for fluoroquinophenoxazine derivatives as possibly new potent topoisomerase I inhibitor. Abstract Text:

Da-Hye Kang,Jung-Sook Kim,Mi-Ja Jung,Eung-Seok Lee,Yurngdong Jahng,Youngjoo Kwon,Younghwa Na,

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 microM, respectively). But compound 8 inhibited topoisomerase I function more selectively at lower concentration, 2 microM. Our observation might strongly implicate that fluoroquinophenoxazines can be developed as efficient topoisomerase I inhibitor with the elaborate modification.

New insight for fluoroquinophenoxazine derivatives as possibly new potent topoisomerase I inhibitor. Publishing Authors By Initials

DH Kang,JS Kim,MJ Jung,ES Lee,Y Jahng,Y Kwon,Y Na,

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New insight for fluoroquinophenoxazine derivatives as possibly new potent topoisomerase I inhibitor. Journal Published:

PUBLICATION TYPE: Research Support, Non-U.S. Gov

Journal: Bioorganic & medicinal chemistry letters

VOLUME: 18

Page Numbers: 1520-4

Journal Abbreviation: Bioorg. Med. Chem. Lett.

ISSN: 1464-3405

DAY: 25

MONTH: 12

YEAR: 2007

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LANGUAGE: eng

NlmUniqueID: 9107377

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Grant and Affiliation Information for New insight for fluoroquinophenoxazine derivatives as possibly new potent topoisomerase I inhibitor.

AFFILIATION: College of Pharmacy, Ewha Womans University, Seoul 120-750, Republic of Korea.

Country: England

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MEDLINETA: Bioorg Med Chem Lett

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