Design, synthesis and biological evaluation of a series of new resveratrol analogues as potential anti-cancer agents

Autor: Lifang Yang, Xuemei Qin, Hongcun Liu, Yanye Wei, Hailiang Zhu, Mingguo Jiang
Jazyk: angličtina
Rok vydání: 2019
Předmět:
Zdroj: Royal Society Open Science, Vol 6, Iss 9 (2019)
Druh dokumentu: article
ISSN: 2054-5703
DOI: 10.1098/rsos.190125
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: Directory of Open Access Journals