Novel palladium (II) complexes with tetradentate thiosemicarbazones. Synthesis, characterization, in vitro cytotoxicity and xanthine oxidase inhibition


ÖZERKAN D., ERTİK O., KAYA B., Kuruca S. E. , YANARDAĞ R., ÜLKÜSEVEN B.

INVESTIGATIONAL NEW DRUGS, cilt.37, ss.1187-1197, 2019 (SCI İndekslerine Giren Dergi) identifier identifier identifier

  • Cilt numarası: 37 Konu: 6
  • Basım Tarihi: 2019
  • Doi Numarası: 10.1007/s10637-019-00751-1
  • Dergi Adı: INVESTIGATIONAL NEW DRUGS
  • Sayfa Sayıları: ss.1187-1197

Özet

In vitro cytotoxicity and xanthine oxidase inhibition capabilities were investigated for five palladium (II) chelate complexes. The palladium complexes were synthesized by starting from S-alkyl-thiosemicarbazones where the alkyl component is methyl, ethyl, propyl or butyl. The solid complexes are characterized by elemental analysis and spectroscopic techniques (UV-visible, IR and 1H NMR). In order to be able to verify the N2O2-type thiosemicarbazidato ligand (L2-) structure in the square planar geometry, complex 1 has been studied as a representative by using single crystal X-ray crystallography. The in vitro cytotoxic activity measurements were carried out in HepG2 and Hep3B hepatocellular carcinomas, HCT116 colorectal carcinoma, and 3 T3 mouse fibroblast cell lines. The palladium complexes exhibited notable cytotoxic activities in all cell lines at lower mu M concentrations compared to the standard chemicals, cisplatin and allopurinol. IC50 values were determined between 0.42 +/- 0.01 and 12.01 +/- 0.37 mu g/ml in examining the antixanthine oxidase abilities of the complexes. Two complexes with S-methyl group exhibited a high inhibition activity on the xanthine oxidase. The results indicated that these complexes could be used as active pharmaceutical ingredients.