Journal
ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY
Volume 18, Issue 4, Pages 529-540Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1871520617666171023142958
Keywords
Human DNA topoisomerase; MTT assay; [H-3]-thymidine incorporation assay; breast cancer cells head and neck squamous cell carcinomas (HNSCC)
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Funding
- Medical University of Lublin [DS.544]
- Ministry of Science and Higher Education [IP2014 037473]
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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 [H-3]-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 topoll. Molecular docking studies proved that 4-benzoyl-1-dichlorobenzoylthiosemicarbazides strongly interact with DNA dependent subunit of that enzyme.
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