Dual Antibacterial and Anticancer Activity of 4-Benzoyl-1-dichlorobenzoylthiosemicarbazide Derivatives

Title:Dual Antibacterial and Anticancer Activity of 4-Benzoyl-1-dichlorobenzoylthiosemicarbazide Derivatives

Volume: 18 Issue: 4

Author(s): Barbara Kapron, Robert Czarnomysy, Agata Paneth, Monika Wujec, Krzysztof Bielawski, Anna Bielawska, Lukasz Swiatek, Barbara Rajtar, Malgorzata Polz-Dacewicz and Tomasz Plech*

Affiliation:

• Department of Pharmacology, Medical University of Lublin, Chodzki 4a, 20-093 Lublin,Poland

Keywords: Human DNA topoisomerase, MTT assay, [3H]-thymidine incorporation assay, breast cancer cells head and neck squamous cell carcinomas (HNSCC).

Abstract: 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.

Cite this article as:

Kapron Barbara , Czarnomysy Robert , Paneth Agata , Wujec Monika , Bielawski Krzysztof , Bielawska Anna , Swiatek Lukasz, Rajtar Barbara , Polz-Dacewicz Malgorzata and Plech Tomasz *, Dual Antibacterial and Anticancer Activity of 4-Benzoyl-1-dichlorobenzoylthiosemicarbazide Derivatives, Anti-Cancer Agents in Medicinal Chemistry 2018; 18 (4) . https://dx.doi.org/10.2174/1871520617666171023142958