Chalcogen-containing phenolics as antiproliferative agents
| Autor: | Paloma Begines, Gabriela B. Plata, José G. Fernández-Bolaños, Inés Maya, Ana Oliete, José M. Padrón, Óscar López |
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| Rok vydání: | 2018 |
| Předmět: |
0301 basic medicine
chemistry.chemical_element Antineoplastic Agents Redox Antioxidants HeLa Structure-Activity Relationship 03 medical and health sciences chemistry.chemical_compound Chalcogen Phenols Dopamine Cell Line Tumor Drug Discovery medicine Humans Cell Proliferation Pharmacology Dose-Response Relationship Drug Molecular Structure biology Chemistry Cell Cycle Glutathione Cell cycle biology.organism_classification 030104 developmental biology Biochemistry Polyphenol Chalcogens Molecular Medicine Drug Screening Assays Antitumor Reactive Oxygen Species Selenium medicine.drug |
| Zdroj: | Future Medicinal Chemistry. 10:319-334 |
| ISSN: | 1756-8927 1756-8919 |
| Popis: | Aim: The increasing number of cancer cases has stimulated researchers to seek for novel approaches. We have combined two bioactive moieties: a polyphenolic scaffold and an organoselenium motif. Four different families (isothiocyanates/thioureas, and their selenium isosters) derived from dopamine, (±)-norepinephrine and R-epinephrine were accessed. Results: Heterocumulenes derived from dopamine and β-O-methylnoradrenaline were strong antiproliferative agents (GI502, -Ph) on the phenyl ring, were also strong antiproliferative agents, besides exhibiting good antiradical and glutathione peroxidase-like activities. Up to a 14-fold increased activity was achieved compared with classical chemotherapeutic agents, exhibiting also different mechanisms of action (cell cycle assays). Redox analysis on HeLa cells suggested an increase of ROS levels after the incubation period. Conclusion: the combination of organoselenium and phenolic moieties might provide valuable lead compounds with relevant antiproliferative properties. |
| Databáze: | OpenAIRE |
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