In vitro and in vivo antitumor activity of platinum(II) complexes with thiosemicarbazones derived from 2-formyl and 2-acetyl pyridine and containing ring incorporated at N(4)-position: Synthesis, spectroscopic study and crystal structure of platinum(II) complexes with thiosemicarbazones, potential anticancer agents
Φόρτωση...
Ημερομηνία
Συγγραφείς
Kovala-Demertzi, D.
Papageorgiou, A.
Papathanasis, L.
Alexandratos, A.
Dalezis, P.
Miller, J. R.
Demertzis, M. A.
Τίτλος Εφημερίδας
Περιοδικό ISSN
Τίτλος τόμου
Εκδότης
Περίληψη
Τύπος
Είδος δημοσίευσης σε συνέδριο
Είδος περιοδικού
peer reviewed
Είδος εκπαιδευτικού υλικού
Όνομα συνεδρίου
Όνομα περιοδικού
Eur J Med Chem
Όνομα βιβλίου
Σειρά βιβλίου
Έκδοση βιβλίου
Συμπληρωματικός/δευτερεύων τίτλος
Περιγραφή
Reactions of thiosemicarbazones of 2-formyl and 2-acetyl pyridine and containing an azepane ring (hexamethyleneiminyl ring) incorporated at N(4)-position, HL(1) (1) and HL(2) (2) with platinum(II) afforded the complexes, [Pt(L(1))Cl] (3) and [Pt(L(2))Cl] (4). Characterization of the compounds was accomplished by means of elemental analysis and spectroscopic techniques NMR, UV-vis and IR spectroscopy. The single-crystal X-ray structure of complex [Pt(L(2))Cl] (4) shows that the ligand monoanion coordinates in a planar conformation to the metal via the pyridyl N atom, the imine-N atom, and thiolato S-atom. Compounds 1-4 have been evaluated for antiproliferative activity in vitro against three human cancer cell lines: MCF-7 (human breast cancer cell line), T24 (bladder cancer cell line), A-549 (non-small cell lung carcinoma) and a mouse L-929 (a fibroblast-like cell line cloned from strain L). Ligand 2 exhibited high activity as anticancer agent against all four cancer cell lines, while ligand 1 exhibited selectivity against MCF-7, L-929 cell lines and complex 4 against A-549, T-24 cancer cell lines. Also, the acute toxicity and antitumor activity were evaluated on leukemia P388-bearing mice. Complex 3 afforded five to six cures against leukemia P388. The in vivo results of the antitumor activity show the two platinum complexes as very effective chemotherapeutic antileukemic agents. (C) 2008 Elsevier Masson SAS. All rights reserved.
Περιγραφή
Λέξεις-κλειδιά
platinum(ii) complexes, thiosemicarbazonato complexes, crystal structure, in vitro and in vivo antitumor activity, biological evaluation, palladium(ii) complexes, spectral properties, 4n-ethyl thiosemicarbazone, biological-activity, derivatives, antifungal, assay
Θεματική κατηγορία
Παραπομπή
Σύνδεσμος
<Go to ISI>://000264558600043
http://ac.els-cdn.com/S0223523408003656/1-s2.0-S0223523408003656-main.pdf?_tid=6f56cc5ddf3232eab4924563afc11c7f&acdnat=1333028802_b848f61872e659f14a9e78e239ff2319
http://ac.els-cdn.com/S0223523408003656/1-s2.0-S0223523408003656-main.pdf?_tid=6f56cc5ddf3232eab4924563afc11c7f&acdnat=1333028802_b848f61872e659f14a9e78e239ff2319
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