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Title: Synthesis, cytotoxic activity and DNA-interaction studies of novel anthraquinone-thiosemicarbazones with tautomerizable methylene group
Authors: Marković, Violeta
Janicijevic A.
Stanojkovic, Tatjana
Kolundžija B.
Sladić, Dušan
Vujčić, Miroslava
Janovic, Barbara
Joksović, Ljubinka
Djurdjevic, Predrag
Todorovic N.
Trifunović, Snežana
Joksović, Milan
Issue Date: 2013
Abstract: A series of novel anthraquinone-thiosemicarbazone derivatives in a tautomerizable keto-imine form was synthesized and tested for their in vitro cytotoxic activity against human cancer cells (HeLa, MDA-MB-361, MDA-MB-453, K562, A549) and human normal MRC-5 cells. Several compounds efficiently inhibited cancer cell growth at micromolar concentrations, especially against K562 and HeLa cells. As determined by flow cytometric analysis, anthraquinone-thiosemicarbazone caused significant increase in the number of sub-G1 phase of HeLa cells and apoptosis in a concentration-dependent manner. Also, inhibition of caspase-3, -8, and -9 with specific caspase inhibitors reduced the apoptosis mediated by the tested compounds in HeLa cells. All anthraquinone-thiosemicarbazones exhibit calf thymus DNA-binding activity, but no cleavage of plasmid DNA was observed. © 2013 Elsevier Masson SAS. All rights reserved.
Type: article
DOI: 10.1016/j.ejmech.2013.03.071
ISSN: 0223-5234
SCOPUS: 2-s2.0-84877040246
Appears in Collections:Faculty of Science, Kragujevac

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