Thio-functionalized carbohydrate thiosemicarbazones and evaluation of their anticancer activity

Bioorganic & Medicinal Chemistry Letters
Anna Czubatka-BieńkowskaTomasz Poplawski

Abstract

Thiosemicarbazides and their analogs have shown potential medical applications as antiviral, antibacterial and anticancer drugs. We designed, synthesized and evaluated in vitro anticancer activity against ovarian (A2780), cervix (HeLa), colon (LoVo), breast (MCF-7) and brain (MO59J) human cancer cell lines of seven novel compounds -S-glycosylated thiosemicarbazones. We assessed the cyto- and genotoxic properties of all novel compounds using a variety of methods including comet assay, XTT assay, various fluorescent assays and toxicology PathwayFinder expression array. We tried to evaluate their possible mechanism of action with particular attention to induction of DNA damage and repair, apoptosis, oxidative stress analysis and cellular response in terms of changes in gene expression. The most sensitive cell line was human ovarian cancer. The results revealed that the major activity against A2780 cancer cell line displayed by our compounds is induction of DNA damage. This effect is not associated with apoptosis or oxidative stress induction and the resulting damage will not lead to cell cycle arrest. We also observed up-expression of heat shock related genes and NQO1 gene in response to our compounds. The second effect seems to b...Continue Reading

Citations

Jul 16, 2020·Archiv der Pharmazie·Feng SongMeng Zhou
May 17, 2017·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Małgorzata Korycka-MachałaJarosław Dziadek
Jun 26, 2021·Chemical Record : an Official Publication of the Chemical Society of Japan ... [et Al.]·Alejandro E CristófaloMaría Laura Uhrig

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