In vitro antitumor activity of 2-acetyl pyridine 4N-ethyl thiosemicarbazone and its platinum(II) and palladium(II) complexes

dc.contributor.authorKovala-Demertzi, D.en
dc.contributor.authorBoccarelli, A.en
dc.contributor.authorDemertzis, M. A.en
dc.contributor.authorColuccia, M.en
dc.date.accessioned2015-11-24T16:39:36Z
dc.date.available2015-11-24T16:39:36Z
dc.identifier.issn0009-3157-
dc.identifier.urihttps://olympias.lib.uoi.gr/jspui/handle/123456789/8173
dc.rightsDefault Licence-
dc.subjectcytotoxic effecten
dc.subjectantitumor activity, in vitroen
dc.subjecttumor cell lines (breast, colon, ovary), humanen
dc.subjectcisplatin-refractory/resistant cell linesen
dc.subjectplatinum(ii)en
dc.subjectpalladium(ii)en
dc.subjectthiosemicarbazone complexesen
dc.subjectcarcinoma cell-linesen
dc.subjectcrystal-structureen
dc.subjectcisplatinen
dc.subjectresistanceen
dc.subjectvivoen
dc.subjectdrugen
dc.titleIn vitro antitumor activity of 2-acetyl pyridine 4N-ethyl thiosemicarbazone and its platinum(II) and palladium(II) complexesen
heal.abstractThe reaction of platinum(II) [Pt(II)] or palladium(II) [Pd(II)] with 2-acetyl pyridine 4N-ethyl thiosemicarbazone, HAc4Et (1) results in the complexes [Pt(Ac4Et)2] (2) and [Pd(Ac4Et) 2] ( 3). In a panel of human tumor cell lines of different origins ( breast, colon, and ovary cancers), and containing also cisplatin-refractory/resistant cell lines, the in vitro growth inhibitory effect of 1-3 was compared to that of cisplatin by using the sulforodamine B assay. After a 96-hour continuous treatment, both the thiosemicarbazone HAc4Et and the metal compounds [Pt(Ac4Et) 2] and [Pd(Ac4Et) 2] exhibit very remarkable growth inhibitory activities with mean IC50 values of 0.9 nM (0.22-2.47 n M), 0.7 n M (0.15-2 n M) and 0.5 n M (0.17-1.02 n M), respectively. In contrast, cisplatin shows a markedly lower growth inhibitory potency, the mean IC 50 in the panel being 2.8 mu M (0.2-8 mu M). In addition to their major cell growth inhibitory potency, complexes 1-3 are characterized by a growth inhibitory profile different from that of cisplatin, being active towards cisplatin-refractory tumor cell lines. These findings, along with the ability of completely overcoming acquired cisplatin resistance from either multifocal or reduced uptake origin, confirm the antitumor potential of HAc4Et and support the hypothesis that both [Pt(Ac4Et)(2)] and [Pd(Ac4Et)(2)] complexes can be characterized by cellular pharmacological properties distinctly different from those of cisplatin. Copyright (c) 2007 S. Karger AG, Basel.en
heal.accesscampus-
heal.fullTextAvailabilityTRUE-
heal.identifier.primaryDoi 10.1159/000099986-
heal.identifier.secondary<Go to ISI>://000244747900011-
heal.identifier.secondaryhttp://content.karger.com/ProdukteDB/produkte.asp?doi=10.1159/000099986-
heal.journalNameChemotherapyen
heal.journalTypepeer reviewed-
heal.languageen-
heal.publicationDate2007-
heal.recordProviderΠανεπιστήμιο Ιωαννίνων. Σχολή Θετικών Επιστημών. Τμήμα Χημείαςel
heal.typejournalArticle-
heal.type.elΆρθρο Περιοδικούel
heal.type.enJournal articleen

Αρχεία

Φάκελος/Πακέτο αδειών

Προβολή: 1 - 1 of 1
Φόρτωση...
Μικρογραφία εικόνας
Ονομα:
license.txt
Μέγεθος:
1.74 KB
Μορφότυπο:
Item-specific license agreed upon to submission
Περιγραφή: