Synthesis, crystal structures, and biological evaluation of manganese(II) and nickel(II) complexes of 4-cyclohexyl-1-(1-(pyrazin-2-yl)ethylidene) thiosemicarbazide

被引:47
作者
Li, Ming Xue [1 ,2 ]
Zhang, Li Zhi [1 ]
Zhang, Dong [1 ]
Ji, Bian Sheng [2 ]
Zhao, Jun Wei [1 ]
机构
[1] Henan Univ, Coll Chem & Chem Engn, Inst Mol & Crystal Engn, Kaifeng 475004, Peoples R China
[2] Henan Univ, Key Lab Nat Med & Immune Engn, Kaifeng 475004, Peoples R China
基金
中国国家自然科学基金; 中国博士后科学基金;
关键词
Thiosemicarbazone; Complex; Crystal structure; Cytotoxicity; HETEROCYCLIC SUBSTITUTED THIOSEMICARBAZONES; COPPER(II) COMPLEXES; IRON(III) COMPLEX; IN-VITRO; ANTITUMOR; 2-BENZOYLPYRIDINE; PALLADIUM(II); COBALT(III); PYRIDINE;
D O I
10.1016/j.ejmech.2011.07.009
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
4-Cyclohexyl-1-(1-(pyrazin-2-yl)ethylidene)thiosemicarbazide (HL) and its transition metal complexes formulated as [Mn(L)(2)] (1) and [Ni(L)(2)] (2) have been prepared in 55-75% yield and characterized by elemental analysis, IR, MS, NMR and single-crystal X-ray diffraction studies. Biological activities of the synthesized compounds have been evaluated against selected Gram positive bacteria Bacillus sub fills, Gram negative bacteria Pseudomonas aeruginosa and the K562 leukemia cell line, respectively. The cytotoxicity data suggest that these compounds may be endowed with important biological properties, especially the nickel complex 2 with MIC = 31.2 mu g/mL and IC50 = 0.53 mu M, respectively. Effect of the free ligand and its two complexes on Mitochondria membrane potential (MMP) and PI-associated fluorescence intensity as well as their effect on cell apoptosis in K562 leukemia cell line was also studied. The tested compounds may exert their cytotoxicity activity via induced loss of MMP. (C) 2011 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码:4383 / 4390
页数:8
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