In vitro antitumor activity of 2-acetyl pyridine 4N-ethyl thiosemicarbazone and its platinum(II) and palladium(II) complexes
Φόρτωση...
Ημερομηνία
Συγγραφείς
Kovala-Demertzi, D.
Boccarelli, A.
Demertzis, M. A.
Coluccia, M.
Τίτλος Εφημερίδας
Περιοδικό ISSN
Τίτλος τόμου
Εκδότης
Περίληψη
Τύπος
Είδος δημοσίευσης σε συνέδριο
Είδος περιοδικού
peer reviewed
Είδος εκπαιδευτικού υλικού
Όνομα συνεδρίου
Όνομα περιοδικού
Chemotherapy
Όνομα βιβλίου
Σειρά βιβλίου
Έκδοση βιβλίου
Συμπληρωματικός/δευτερεύων τίτλος
Περιγραφή
The 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.
Περιγραφή
Λέξεις-κλειδιά
cytotoxic effect, antitumor activity, in vitro, tumor cell lines (breast, colon, ovary), human, cisplatin-refractory/resistant cell lines, platinum(ii), palladium(ii), thiosemicarbazone complexes, carcinoma cell-lines, crystal-structure, cisplatin, resistance, vivo, drug
Θεματική κατηγορία
Παραπομπή
Σύνδεσμος
<Go to ISI>://000244747900011
http://content.karger.com/ProdukteDB/produkte.asp?doi=10.1159/000099986
http://content.karger.com/ProdukteDB/produkte.asp?doi=10.1159/000099986
Γλώσσα
en
Εκδίδον τμήμα/τομέας
Όνομα επιβλέποντος
Εξεταστική επιτροπή
Γενική Περιγραφή / Σχόλια
Ίδρυμα και Σχολή/Τμήμα του υποβάλλοντος
Πανεπιστήμιο Ιωαννίνων. Σχολή Θετικών Επιστημών. Τμήμα Χημείας