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Investigational New Drugs
Published in: Investigational New Drugs 6/2019

01-12-2019 | Xanthine Alkaloid | PRECLINICAL STUDIES

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

Authors: Dilşad Özerkan, Onur Ertik, Buşra Kaya, Serap Erdem Kuruca, Refiye Yanardag, Bahri Ülküseven

Published in: Investigational New Drugs | Issue 6/2019

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Summary

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 μM concentrations compared to the standard chemicals, cisplatin and allopurinol. IC50 values were determined between 0.42 ± 0.01 and 12.01 ± 0.37 μg/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.
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Metadata
Title
Novel palladium (II) complexes with tetradentate thiosemicarbazones. Synthesis, characterization, in vitro cytotoxicity and xanthine oxidase inhibition
Authors
Dilşad Özerkan
Onur Ertik
Buşra Kaya
Serap Erdem Kuruca
Refiye Yanardag
Bahri Ülküseven
Publication date
01-12-2019
Publisher
Springer US
Published in
Investigational New Drugs / Issue 6/2019
Print ISSN: 0167-6997
Electronic ISSN: 1573-0646
DOI
https://doi.org/10.1007/s10637-019-00751-1

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