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Dihydroxylated 2,4,6-triphenyl pyridines: Synthesis, topoisomerase i and II inhibitory activity, cytotoxicity, and structure-activity relationship study

Title
Dihydroxylated 2,4,6-triphenyl pyridines: Synthesis, topoisomerase i and II inhibitory activity, cytotoxicity, and structure-activity relationship study
Authors
Karki R.Thapa P.Yoo H.Y.Kadayat T.M.Park P.-H.Na Y.Lee E.Jeon K.-H.Cho W.-J.Choi H.Kwon Y.Lee E.-S.
Ewha Authors
권영주
SCOPUS Author ID
권영주scopus
Issue Date
2012
Journal Title
European Journal of Medicinal Chemistry
ISSN
0223-5234JCR Link
Citation
vol. 49, pp. 219 - 228
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
Twelve dihydroxylated 2,4,6-triphenyl pyridines were designed and synthesized which contain hydroxyl groups at ortho, meta or para position of 2- and 6-phenyl, or 2- and 4-phenyl rings attached to the central pyridine. They were evaluated for topoisomerase I and II inhibitory activity, and cytotoxicity against several human cancer cell lines for the development of novel anticancer agents. Generally, dihydroxylated 2,4,6-triphenyl pyridines exhibited stronger topoisomerase II inhibitory activity, and cytotoxicity compared to those of monohydroxylated 2,4,6-triphenyl pyridines. The concrete structure-activity relationship was observed that dihydroxylated 2,4,6-triphenyl pyridines with hydroxyl group at meta or para position of 2-phenyl ring displayed significant topoisomerase II inhibitory activity as well as cytotoxicity. Positive correlation between topoisomerase II inhibitory activity and cytotoxicity was observed for compounds 10, 12, 13, 17-20 and 22. © 2012 Elsevier Masson SAS. All rights reserved.
DOI
10.1016/j.ejmech.2012.01.015
Appears in Collections:
약학대학 > 약학과 > Journal papers
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