4.7 Article

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

期刊

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 46, 期 9, 页码 4383-4390

出版社

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2011.07.009

关键词

Thiosemicarbazone; Complex; Crystal structure; Cytotoxicity

资金

  1. National Natural Science Foundation of China [21071043]
  2. China Postdoctoral Science Foundation [20090460847]
  3. Foundation for University Young Key Teacher by Henan Province [2009GGJS-025]
  4. Natural Science Foundation of the Educational Department of Henan Province [2010B150003]

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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.

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