<p>The present study aims at the synthesis of Schiff base-containing platinum(II) complexes with a general formula of [Pt(ketone)<sub>2</sub>A(L<sub>2</sub>)], where ketones are 2-heptanone, 2-octanone or 3-octanone; <i>A</i> is hydrazine, phenylhydrazine or o-phenylene-diamine; <i>L</i> is 1-naphthylamine, 2-amino-pyrimidine, 2-methylimidazole or 2-amino-4-methylpyridine. The complexes were obtained from reactions between PtCl<sub>2</sub>, ketones and amine compounds in appropriate solvents. A detailed analysis of the physicochemical properties of the complexes was accomplished using: Fourier-transform infrared (FTIR) spectroscopy, thermal analysis (TA), mass spectrometry (MS), nuclear magnetic resonance (NMR), UV–Vis spectroscopy, powder X-ray diffraction (XRD), scanning electron microscopy (SEM) and energy-dispersive X-ray (EDX) spectroscopy. The biological effects of some selected complexes on the Gram-positive bacteria strain <i>Staphylococcus aureus</i> and on normal and tumor cells were also investigated. Two complexes (C3 and C9) showed antibacterial activity, the inhibitory effect being dependent on the concentrations applied. Two compounds (C2 and C9) exhibited antitumoral activity against two ovarian cancer cell lines, through increased cytotoxicity cellular death (mostly by late apoptosis) and DNA damage. The compound C2 affected also platinum-resistant tumor cells. These effects were milder on normal cells, suggesting a possible protective effect on healthy tissues. The results highlight the potential utility of this class of compounds in medicinal chemistry and the importance of testing them in further studies to ascertain their application as future antibacterial and/or anticancer drugs.</p>

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Novel Schiff base-type platinum(II) complexes: syntheses, physical–chemical characterization and biological activities

  • Cs. Várhelyi Jr.,
  • R. A. Mereu,
  • R. Szalay,
  • J. Madarász,
  • J. Papp,
  • J. Mihály,
  • M. Simon-Várhelyi,
  • I. Brie,
  • C. Tatomir,
  • O. Sava,
  • Zs. Fekete,
  • Á. Vajda,
  • P. Virág

摘要

The present study aims at the synthesis of Schiff base-containing platinum(II) complexes with a general formula of [Pt(ketone)2A(L2)], where ketones are 2-heptanone, 2-octanone or 3-octanone; A is hydrazine, phenylhydrazine or o-phenylene-diamine; L is 1-naphthylamine, 2-amino-pyrimidine, 2-methylimidazole or 2-amino-4-methylpyridine. The complexes were obtained from reactions between PtCl2, ketones and amine compounds in appropriate solvents. A detailed analysis of the physicochemical properties of the complexes was accomplished using: Fourier-transform infrared (FTIR) spectroscopy, thermal analysis (TA), mass spectrometry (MS), nuclear magnetic resonance (NMR), UV–Vis spectroscopy, powder X-ray diffraction (XRD), scanning electron microscopy (SEM) and energy-dispersive X-ray (EDX) spectroscopy. The biological effects of some selected complexes on the Gram-positive bacteria strain Staphylococcus aureus and on normal and tumor cells were also investigated. Two complexes (C3 and C9) showed antibacterial activity, the inhibitory effect being dependent on the concentrations applied. Two compounds (C2 and C9) exhibited antitumoral activity against two ovarian cancer cell lines, through increased cytotoxicity cellular death (mostly by late apoptosis) and DNA damage. The compound C2 affected also platinum-resistant tumor cells. These effects were milder on normal cells, suggesting a possible protective effect on healthy tissues. The results highlight the potential utility of this class of compounds in medicinal chemistry and the importance of testing them in further studies to ascertain their application as future antibacterial and/or anticancer drugs.