Abstract
The preliminary cytotoxic effect of 4-ethoxycarbonylmethyl-1-(piperidin-4-ylcarbonyl)-thiosemicarbazide hydrochloride (1)-a potent topoisomerase II inhibitor-was measured using a MTT assay. It was found that the compound decreased the number of viable cells in both estrogen receptor-positive MCF-7 and estrogen receptor-negative MDA-MB-231breast cancer cells, with IC(50) values of 146 ± 2 and 132 ± 2 μM, respectively. To clarify the molecular basis of the inhibitory action of 1, molecular docking studies were carried out. The results suggest that 1 targets the ATP binding pocket.
MeSH terms
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Adenosine Triphosphate / metabolism*
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Breast Neoplasms / drug therapy*
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Cell Line, Tumor
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Cell Survival / drug effects
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DNA Topoisomerases, Type II / metabolism*
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Drug Screening Assays, Antitumor
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Female
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Humans
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MCF-7 Cells
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Molecular Docking Simulation
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Piperidines / metabolism
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Piperidines / pharmacology*
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Semicarbazides / metabolism
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Semicarbazides / pharmacology*
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Topoisomerase II Inhibitors / metabolism
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Topoisomerase II Inhibitors / pharmacology*
Substances
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4-ethoxycarbonylmethyl-1-(piperidin-4-ylcarbonyl)thiosemicarbazide
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Piperidines
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Semicarbazides
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Topoisomerase II Inhibitors
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thiosemicarbazide
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Adenosine Triphosphate
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DNA Topoisomerases, Type II