Design, synthesis and biological evaluation of a series of new resveratrol analogues as potential anti-cancer agents
| Autor: | Hong-Cun Liu, Wei Yanye, Xuemei Qin, Lifang Yang, Mingguo Jiang, Hai-Liang Zhu |
|---|---|
| Rok vydání: | 2019 |
| Předmět: |
genetic structures
Resveratrol resveratrol behavioral disciplines and activities 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine medicine lcsh:Science anti-cancer 030304 developmental biology Biological evaluation 0303 health sciences Multidisciplinary biology Chemistry Cancer synthesis of resveratrol analogues molecular docking medicine.disease Tubulin nervous system Biochemistry Design synthesis tubulin 030220 oncology & carcinogenesis biology.protein lcsh:Q psychological phenomena and processes Research Article |
| Zdroj: | Royal Society Open Science, Vol 6, Iss 9 (2019) Royal Society Open Science |
| ISSN: | 2054-5703 |
| Popis: | A series of novel resveratrol derivatives were designed, synthesized and evaluated as anti-cancer agents. Most of the compounds showed significant anti-proliferative activities against three human cancer cell lines (HepG2, A549 and Hela). Among these compounds, compound r displayed the most potent inhibitory activity and showed low cytotoxic activity. Cell apoptosis and cell cycle assays demonstrated that compound r significantly induced apoptosis ( p < 0.001) and arrested cell cycle at S phase. Immunofluorescence microscopy analysis showed compound r disrupted the tubulin network. Docking simulations supported the pharmacological results of compound r . It is believed that this work would be very useful for designing a new series of tubulin inhibitors. |
| Databáze: | OpenAIRE |
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