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
Author(s)
이응석타라만카다얏박찬미[박찬미]전규연[전규연]틸바하두르다빠마가르유한영권영주[권영주]비스트가네쉬
Keywords
DNA TOPOISOMERASES; 2,4,6-TRISUBSTITUTED PYRIDINE; 2,4,6-TRIPHENYL PYRIDINES; BREAST-CANCER; IN-VITRO; CYTOTOXICITY; COMPLEXES; MOIETY; DESIGN; POTENT
Issue Date
201501
Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
Citation
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v.90, pp.302 - 314
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.
URI
http://hdl.handle.net/YU.REPOSITORY/33728http://dx.doi.org/10.1016/j.ejmech.2014.11.046
ISSN
0223-5234
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약학대학 > 약학부 > Articles
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