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Design, docking, and synthesis of novel indeno[1,2-c]isoquinolines for the development of antitumor agents as topoisomerase I inhibitors

Title
Design, docking, and synthesis of novel indeno[1,2-c]isoquinolines for the development of antitumor agents as topoisomerase I inhibitors
Authors
Cho W.-J.Le Q.M.My Van H.T.Youl Lee K.Kang B.Y.Lee E.-S.Lee S.K.Kwon Y.
Ewha Authors
이상국권영주
SCOPUS Author ID
권영주scopus
Issue Date
2007
Journal Title
Bioorganic and Medicinal Chemistry Letters
ISSN
0960-894XJCR Link
Citation
vol. 17, no. 13, pp. 3531 - 3534
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
An intramolecular radical cyclization reaction of 4-bromo-3-arylisoquinolines 11a-c allowed the efficient synthesis of 11-methylindenoisoquinolines 2a-c. 5-(2-Aminoethylamino)indeno[1,2-c]isoquinolin-11-one 4 was also prepared in the convenient manner. The synthesized compounds were tested in vitro for cytotoxicity and DNA-topoisomerase 1 (top 1) inhibitory activity. The dramatic enhancement of top 1 inhibitory activity of 4 was explained by a docking study using the FlexX program. © 2007 Elsevier Ltd. All rights reserved.
DOI
10.1016/j.bmcl.2007.04.064
Appears in Collections:
약학대학 > 약학과 > Journal papers
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