Journal of Inorganic Biochemistry ( IF 3.9 ) Pub Date : 2020-07-31 , DOI: 10.1016/j.jinorgbio.2020.111205 Tarlok S Lobana 1 , Mani Kaushal 1 , Ritu Bala 1 , Lovedeep Nim 2 , Kamaldeep Paul 3 , Daljit S Arora 2 , Astha Bhatia 4 , Saroj Arora 4 , Jerry P Jasinski 5
The basic aim of this study pertains to developing antimicrobial or anticancer agents based on N, S-donor organic ligands bonded to metals. In the present investigation, di-2-pyridylketone-N1-substituted thiosemicarbazone (py2tscH-N1HR2, Chart 2) thio-ligands were reacted with copper(I) halides in organic solvents yielding copper(II) complexes of stoichiometry, [Cu(N,N,S-py2tsc-N1HR2)X] (X = I, R2 = H, 1; Me, 2; Et, 3; Ph, 4; X = Br, R2 = H, 5; Me, 6; Et, 7; Ph, 8; X = Cl, R2 = H, 9; Me, 10; Et, 11; Ph, 12); the formation of CuII probably occurs through a proton coupled electron transfer (PCET) process. Electron spin resonance, ultraviolet-visible spectroscopy and X-ray crystallography (2, 3, 5, 7, 11) supported a distorted square planar geometry of these complexes. Moderate to high antimicrobial activities of these complexes against methicillin resistant Staphylococcus aureus, Gram positive bacteria, Staphylococcus aureus and Gram negative bacteria, Klebsiella pneumoniae 1, Salmonella typhimurium 2 and one yeast Candida albicans were recorded. Complexes were found to be biosafe with 88–91% cellular viability. All complexes have shown high anticancer activity against the immortalized L6 rat skeletal muscle cell line with very low IC50 values.
中文翻译:
铜 (II) 的二-2-吡啶基酮-N1-取代的缩氨基硫脲衍生物:对永生化 L6 大鼠骨骼肌细胞的生物安全抗菌潜力和高抗癌活性。
本研究的基本目的是开发基于与金属结合的 N、S 供体有机配体的抗菌或抗癌剂。在本研究中,二-2-吡啶基酮-N 1 -取代的氨基硫脲(py 2 tscH-N 1 HR 2,图2)硫代配体在有机溶剂中与卤化铜(I)反应,生成铜(II)配合物化学计量,[Cu(N,N,S-py 2 tsc-N 1 HR 2 )X] (X = I, R 2 = H, 1 ; Me, 2 ; Et, 3; Ph, 4 ; X = Br, R 2 = H, 5 ; 我, 6; ET, 7 ; 博士, 8 ; X = Cl, R 2 = H, 9;我,10;等,11;博士, 12 ); Cu II的形成可能是通过质子耦合电子转移 (PCET) 过程发生的。电子自旋共振、紫外-可见光谱和 X 射线晶体学 ( 2 , 3 , 5 , 7 , 11 ) 支持这些复合物的扭曲方形平面几何形状。这些复合物对耐甲氧西林金黄色葡萄球菌、革兰氏阳性菌、记录了金黄色葡萄球菌和革兰氏阴性菌、肺炎克雷伯菌1、鼠伤寒沙门氏菌2 和一种酵母白色念珠菌。发现复合物具有 88-91% 的细胞活力,具有生物安全性。所有复合物均显示出对永生化 L6 大鼠骨骼肌细胞系的高抗癌活性,IC 50值非常低。