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Synthesis, electronic structure and molecular docking of new organometallic palladium (II) complexes with intercalator lignads: The influence of bridged ligands on enhanced DNA/serum protein binding and in vitro antitumoral activity

Publication date:

1 January 2017


Source:Journal of Organometallic Chemistry, Volume 827

Author(s): Kazem Karami, Zohreh Mehri Lighvan, Maryam Dehdashti Jahromi, Janusz Lipkowski, Amir Abbas Momtazi-borojeni

Novel organometallic palladium(II) complexes [Pd2{(C,N)C12H8NH2)}2(μ-dppf)Cl2] (2) [Pd2{(C,N)C12H8NH2)}2(μ-dpp)Cl2] (3) [1,1-bis(diphenylphosphine)-ferrocene (dppf), 1,3-Bis(4-pyridyl)propane (bpp)] have been synthesized, fully characterized by elemental analysis, multi-nuclear (1H,31P{1H},13C{1H}) NMR and IR spectroscopic techniques and their biological activities such as anti-tumoral activity and DNA-protein interactions have been investigated. The crystal structure of (2), established by X-ray diffraction, shows that the dppf ligand is bound to the two palladium atoms in bridged form. The interaction of the complexes with calf thymus DNA (CT-DNA) has been explored by UV–Vis spectroscopy, emission titration and thermal denaturation (Tm) methods, which have revealed that these complexes interact with DNA through intercalation mode. Competitive studies with methylene blue (MB) have shown the ability of the complexes to displace the DNAbound MB, suggesting a competition with MB. Furthermore, the microenvironment and the secondary structure of BSA are changed in the presence of the complexes. Competitive binding using Warfarin, Digoxin and site markers, which have definite binding sites, demonstrated that the complexes bind to site I on BSA. Notably, the complexes exhibit significant in vitro selective cytotoxicity against two human cancer cell lines (JURKAT and SKOV3) with IC50 values varying from 2.3 to 6.7 μM. This indicates that they are more active than cisplatin and showing low cytotoxic activity on normal cells. Finally, molecular modelling studies have been conducted to determine the binding site of the DNA and BSA with the complexes.
Graphical abstract




Authors:   Author(s): Kazem Karami, Zohreh Mehri Lighvan, Maryam Dehdashti Jahromi, Janusz Lipkowski, Amir Abbas Momtazi-borojeni
Journal:   Journal of Organometallic Chemistry
Year:   2016
Publication date:   06-Nov-2016
Facts, background information, dossiers
  • cisplatin
  • cells
  • cell lines
  • Binding Site
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