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In vitro anticancer activity of gold(III) complexes with some esters of (S,S)-ethylenediamine-N,N '-di-2-propanoic acid

Authorized Users Only
2015
Authors
Pantelić, Nebojša
Stanojković, Tatjana P.
Zmejkovski, Bojana B.
Sabo, Tibor J.
Kaludjerović, Goran N.
Article (Published version)
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Abstract
Five novel gold(III) complexes of general formulas [AuCl2{(S,S)-R(2)eddip}]PF6, ((S,S)-eddip = (S,S)-ethylenediamine-N,N'-di-2-propanoate, R = n-Bu, n-Pe, i-Bu, i-Am, cPe; 1-5, respectively) were synthesized and characterized by UV/Vis, IR and NMR spectroscopy and mass spectrometry. DFT calculations indicated that (R,R)-N,N'-configuration diastereoisomers were the most stable for 1-5. 3 is stable in DMSO for at least 24 h, but immediate hydrolysis in PBS occurs. 3 is readily reduced with ascorbic acid and forms adducts with bovine serum albumin (BSA). In vitro anticancer activity of the gold(III) complexes against human cervix adenocarcinoma HeLa, human myelogenous leukemia K562, human melanoma Fem-x tumor cell lines, as well as against non-cancerous human embryonic lung fibroblast cell line MRC5 was determined using MIT assay. Complex 4 showed highest activity and selectivity (IC50(Femx) = 1.3 +/- 0.2; IC50(MRC-5)/IC50(Fem-x) = 72.5 +/- 12.4), 4 times more active and 28 times more sel...ective than cisplatin. Complexes induced apoptotic mode of death in a time-dependent manner in HeLa cells.

Keywords:
Gold(III) complexes / R(2)edda-type ligands / DFT / Apoptosis / Cell cycle / Cytotoxicity
Source:
European Journal of Medicinal Chemistry, 2015, 90, 766-774
Publisher:
  • Elsevier France-Editions Scientifiques Medicales Elsevier, Issy-Les-Moulineaux
Funding / projects:
  • Rational design and synthesis of biologically active and coordination compounds and functional materials, relevant for (bio)nanotechnology (RS-172035)
  • Biological response modifiers in physiological and pathological conditions (RS-175011)

DOI: 10.1016/j.ejmech.2014.12.019

ISSN: 0223-5234

PubMed: 25528331

WoS: 000348951900060

Scopus: 2-s2.0-84918804131
[ Google Scholar ]
URI
http://aspace.agrif.bg.ac.rs/handle/123456789/3779
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  • Radovi istraživača / Researchers’ publications
Institution/Community
Poljoprivredni fakultet

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