Department of Genetic and Bioengineering, Faculty of Engineering and Architecture, Kastamonu University, Kastamonu, Turkey.
Department of Chemistry, Engineering Faculty, Istanbul University-Cerrahpasa, 34320, Avcilar, Istanbul, Turkey.
Invest New Drugs. 2019 Dec;37(6):1187-1197. doi: 10.1007/s10637-019-00751-1. Epub 2019 Mar 14.
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. IC 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.
采用 S-烷基缩氨硫脲为起始原料,合成了 5 种钯(II)螯合物。钯配合物通过元素分析和光谱技术(UV-可见、IR 和 1H NMR)进行了表征。为了能够在四方平面几何结构中验证 N2O2 型缩氨硫脲配体(L2-)结构,选择了配合物 1 作为代表进行了单晶 X 射线晶体学研究。在 HepG2 和 Hep3B 肝癌、HCT116 结直肠癌和 3T3 小鼠成纤维细胞系中进行了体外细胞毒性测定。与标准化学物质顺铂和别嘌呤醇相比,钯配合物在较低的 μM 浓度下在所有细胞系中表现出显著的细胞毒性活性。在检测复合物的抗黄嘌呤氧化酶能力时,IC 值在 0.42±0.01 和 12.01±0.37 μg/ml 之间。两个具有 S-甲基基团的配合物对黄嘌呤氧化酶表现出高抑制活性。结果表明,这些配合物可用作活性药物成分。