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Title: Synthesis and evaluation of series of diazine-bridged dinuclear platinum(II) complexes through in vitro toxicity and molecular modeling: Correlation between structure and activity of pt(II) complexes
Authors: Senerovic, Lidija
Zivkovic, Marija
Veselinovic, Aleksandar
Pavic A.
Djuran, Miloš
Rajković, Snežana
Nikodinovic-Runic, Jasmina
Issue Date: 2015
Abstract: © 2014 American Chemical Society. Polynuclear Pt(II) complexes are a novel class of promising anticancer agents with potential clinical significance. A series of pyrazine (pz) bridged dinuclear Pt(II) complexes with general formulas {[Pt(L)Cl]<inf>2</inf>(μ-pz)}<sup>2+</sup> (L, ethylenediamine, en; (±)-1,2-propylenediamine, 1,2-pn; isobutylenediamine, ibn; trans-(±)-1,2-diaminocyclohexane, dach; 1,3-propylenediamine, 1,3-pd; 2,2-dimethyl-1,3-propylenediamine, 2,2-diMe-1,3-pd) and one pyridazine (pydz) bridged {[Pt(en)Cl]<inf>2</inf>(μ-pydz)}<sup>2+</sup> complex were prepared. The anticancer potential of these complexes were determined through in vitro cytotoxicity assay in human fibroblasts (MRC5) and two carcinoma cell lines (A375 and HCT116), interaction with double stranded DNA through in vitro assay, and molecular docking study. All complexes inhibited cell proliferation with inhibitory concentrations in the 0.5-120 μM range. While {[Pt(1,3-pd)Cl]<inf>2</inf>(μ-pz)}<sup>2+</sup> showed improved activity and {[Pt(en)Cl]<inf>2</inf>(μ-pydz)}<sup>2+</sup> showed comparable activity to that of clinically relevant cisplatin, {[Pt(en)Cl]<inf>2</inf>(μ-pydz)}<sup>2+</sup> was less toxic in an assay with zebrafish (Danio rerio) embryos, causing no adverse developmental effects. The in vitro cytotoxicity of all diazine-bridged dinuclear Pt(II) complexes is discussed in correlation to their structural characteristics.
Type: article
DOI: 10.1021/jm5017686
ISSN: 0022-2623
SCOPUS: 2-s2.0-84922826336
Appears in Collections:Faculty of Medical Sciences, Kragujevac
Faculty of Science, Kragujevac

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