Diversity-oriented synthesis of cembranoid derivatives as potential anti-inflammatory agents
Cong Zhang, Heng Li, Jin Liu, Moting Liu, Hao Zhang, Kai-Xian Chen, Yue-Wei Guo, Wei Tang, Xu-Wen Li
Journal：BIOORGANIC CHEMISTRY
IF：5.28
DOI：10.1016/j.bioorg.2021.104887
PMID：33865055
Published：2021-04-06
research field：分子生物学植物学植物遗传学采后生理学活性氧代谢
Abstract
Eleven novel cembranoid derivatives were designed, synthesized, and evaluated for their inflammation related activities on the basis of our isolated and previously reported anti-inflammatory marine cembranoids. In bioassay, compound 11 displayed the most promising inhibitory effects with IC 50 value of 1.1 μM for the TNF-α inhibitory activity. The further mechanism study of 11 on the inflammatory signaling transduction of RAW264.7 cells was also performed. This research may give an insight for the discovery of marine cembranoid derived anti-inflammatory drug leads.
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