Dalton Transactions · 2022 · 12 citations · 36 references
PharmacyMedicinal ChemistryPharmacologyCancer PharmacologyDrug DiscoveryRedox BiochemistryReactive Oxygen SpeciesRedox ChemistryClick Chemistry FunctionalizationClick-chemistry LinkersHydrogen Peroxide GenerationMedicinal Chemistry ApplicationsRedox-active LigandsSpin TrappingTriazole ChemistryVoltammetry
studies in MCF-7 breast cancer cells show significant increases in ROS following incubation with the Fc-functionalized compounds. Screening for antibacterial activity produced negative results for all of the Fc compounds, consitent with low levels of hydrogen peroxide typically found in bacteria. By contrast, Fc-coumarin showed cytotoxicity against A549 lung cancer and SKOV3 ovarian cancer cell lines, whereas the parent compound was inactive. This is consistent both with the cytoxic potential of the Fc group and the elevated hydrogen peroxide levels found in many cancers. Interestingly, the anthraquinone compounds showed the opposite effect with the parent compounds showing modest activity against A549 cells, but the Fc compounds being inactive. This demonstrates other potential negative impacts of including Fc, such as significantly increased lipophilicity.
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