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Hydroxylated 2,4-diphenyl indenopyridine derivatives as a selective non-intercalative topoisomerase II alpha catalytic inhibitor

Title
Hydroxylated 2,4-diphenyl indenopyridine derivatives as a selective non-intercalative topoisomerase II alpha catalytic inhibitor
Authors
Kadayat, Tara ManPark, ChanmiJun, Kyu-YeonMagar, Til Bahadur ThapaBist, GaneshYoo, Han YoungKwon, YoungjooLee, Eung-Seok
Ewha Authors
권영주
SCOPUS Author ID
권영주scopus
Issue Date
2015
Journal Title
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
ISSN
0223-5234JCR Link

1768-3254JCR Link
Citation
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY vol. 90, pp. 302 - 314
Keywords
Hydroxylated 2,4-diphenyl indenopyridineAnticancer agentsTerpyridineTopoisomerase II alpha non-intercalative catalytic inhibitorAntiproliferative activity
Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
Indexed
SCIE; SCOPUS WOS scopus
Document Type
Article
Abstract
For the development of novel anticancer agents, we designed and synthesized hydroxylated 2,4-diphenyl indenopyridines, and evaluated their topoisomerase inhibitory activity as well as their antiproliferative activities against several human cancer cell lines. The structure activity relationship study showed that indenopyridines with hydroxyl group at meta or para positions of 2- or 4- phenyl ring displayed selective and significant topoisomerase II alpha (topo II alpha) inhibitory activity and potent antiproliferative activity. Positive correlation between topo II alpha inhibition and antiproliferative activity was observed for compounds 15, 16, 18-20, 22, 23, 25 and 26. The mode of action of compound 16 was further evaluated to be a non-intercalative topo Ha catalytic inhibitor. (C) 2014 Elsevier Masson SAS. All rights reserved.
DOI
10.1016/j.ejmech.2014.11.046
Appears in Collections:
약학대학 > 약학과 > Journal papers
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