Cytotoxic activity of acridin-3,6-diyl dithiourea hydrochlorides in human leukemia line HL-60 and resistant subline HL-60/ADR |
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| Authors: | Zuzana Vantová Helena Paulíková Danica Sabolová Mária Ko?urková Mária Sucháňová Ladislav Janovec Pavol Kristian Ján Imrich |
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| Institution: | 1. Department of Biochemistry and Microbiology, Faculty of Chemical and Food Technology, Slovak Technical University, Radlinského 9, SK-81237 Bratislava, Slovak Republic;2. Department of Biochemistry, Institute of Chemistry, Faculty of Science, P.J. ?afárik University, Moyzesova 11, SK-04167 Ko?ice, Slovak Republic;3. Department of Organic Chemistry, Institute of Chemistry, Faculty of Science, P.J. ?afárik University, Moyzesova 11, SK-04167 Ko?ice, Slovak Republic |
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| Abstract: | A series of acridin-3,6-diyl dithiourea hydrochloride derivatives (alkyl-AcrDTU) was prepared and tested against sensitive and drug resistant leukemia cell lines for their cytotoxic/cytostatic activity. The products (ethyl-, n-propyl-, n-butyl-, n-pentyl-AcrDTU) showed high DNA binding affinity via intercalation (K = 7.6 ? 2.9 × 105 M?1). All derivatives inhibited proliferation of HL-60 cells and its resistant subline HL-60/ADR, unexpectedly the resistant subline was more sensitive than the parental one (IC50 = 3.5 μM, 48-treatment of HL-60/ADR with pentyl-AcrDTU). Cytotoxicity of tested compounds was associated with their DNA-binding properties and the level of intracellular thiols has been changed in the presence of AcrDTU. |
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