Objective/Method: A group of 4-benzoyl-1-dichlorobenzoylthiosemicarbazides endowed
with antibacterial activity was evaluated for its cytotoxic properties against breast cancer cells (MCF-7,
MDA-MB-231) and head and neck squamous cell carcinomas (FaDu, SCC-25). Cytotoxicity of the investigated
compounds was measured using MTT and [3H]-thymidine incorporation bioassays.
Result: 1-(2,3-Dichlorobenzoyl)-4-(2-methylbenzoyl)thiosemicarbazide (TA-4), 1-(2,4-dichlorobenzoyl)-
4-(2-methylbenzoyl)thiosemicarbazide (TA-18), and 1-(2,4-dichlorobenzoyl)-4-(4-nitrolbenzoyl)-
thiosemicarbazide (TA-20) were found to possess anticancer activity equipotent or even stronger than
that of reference drug – etoposide. In order to clarify the molecular mode of action of the mentioned
compounds, the relaxation assay kit for human DNA topoisomerase II was used. It turned out that reduction
of viability of cancer cells was a result of inhibition of human DNA topoII. Molecular docking
studies proved that 4-benzoyl-1-dichlorobenzoylthiosemicarbazides strongly interact with DNAdependent
subunit of that enzyme.