| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1987862 | International Journal of Biological Macromolecules | 2009 | 7 Pages |
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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Authors
Zuzana Vantová, Helena Paulíková, Danica Sabolová, Mária Kožurková, Mária Sucháňová, Ladislav Janovec, Pavol Kristian, Ján Imrich,