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Title: Antiproliferative activity and QSAR studies of a series of new 4-aminomethylidene derivatives of some pyrazol-5-ones
Authors: Marković, Violeta
Erić J.
Stanojkovic, Tatjana
Gligorijevic N.
Arandelović I.
Todorovic N.
Trifunović, Snežana
Manojlovic, Nedeljko
Jelic, Ratomir
Joksović, Milan
Journal: Bioorganic and Medicinal Chemistry Letters
Issue Date: 1-Aug-2011
Abstract: Twenty five 4-aminomethylidene derivatives obtained from 3-phenyl-2-pyrazolin-5-one and 1,3-diphenyl-2-pyrazolin-5-one were synthesized and tested for their antiproliferative activity against human breast cancer MDA-MB-361 and MDA-MB-453 cell lines. The compounds derived from 1,3-diphenyl-2-pyrazolin-5-one exhibited the most remarkable activity in the treatment of both cell lines. In vitro antiproliferative activities were accompanied by an important apoptotic fraction of both cell lines; also, compounds inhibited key endothelial cell functions implicated in invasion and angiogenesis. QSAR methods were performed in order to analyze the influence of structural features of the compounds investigated on the antiproliferative potential on MDA-MB-361 and MDA-MB-453 cancer cells. One-parameter heuristic analysis was performed and different whole molecule and fragmental descriptors were considered for rationalization of mechanism of interaction of these compounds with active place of hypothetical target included in tumorigenesis. © 2011 Elsevier Ltd. All rights reserved.
Type: Article
DOI: 10.1016/j.bmcl.2011.06.025
ISSN: 0960894X
SCOPUS: 79960347940
Appears in Collections:Faculty of Medical Sciences, Kragujevac
Faculty of Science, Kragujevac
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