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Cembranoid Derivatives as Anti-Inflammatory Agents: Synthesis and Activity | 翌圣生物
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：肿瘤学药理学药物化学有机合成药物发现
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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