Novel palladium (II) complexes with tetradentate thiosemicarbazones. Synthesis, characterization, in vitro cytotoxicity and xanthine oxidase inhibition
INVESTIGATIONAL NEW DRUGS, cilt.37, sa.6, ss.1187-1197, 2019 (SCI-Expanded, Scopus)
- Yayın Türü: Makale / Tam Makale
- Cilt numarası: 37 Sayı: 6
- Basım Tarihi: 2019
- Doi Numarası: 10.1007/s10637-019-00751-1
- Dergi Adı: INVESTIGATIONAL NEW DRUGS
- Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
- Sayfa Sayıları: ss.1187-1197
- Anahtar Kelimeler: Palladium, Thiosemicarbazone, X-ray analysis, Cytotoxicity, Xanthine oxidase, RIBONUCLEOTIDE REDUCTASE INHIBITOR, METAL-COMPLEXES, PHASE-I, CANCER, ANTIBACTERIAL, DERIVATIVES, LIGANDS, DNA, ANTIFUNGAL, CHLORIDE
- İstanbul Üniversitesi-Cerrahpaşa Adresli: Evet
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.