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Diversity-oriented synthesis of cembranoid derivatives as potential anti-inflammatory agents. 2021
Cong Zhang, and
Heng Li, and
Jin Liu, and
Moting Liu, and
Hao Zhang, and
Kai-Xian Chen, and
Yue-Wei Guo, and
Wei Tang, and
Xu-Wen Li
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Zhangjiang Hi-Tech Park, Shanghai 201203, China; Nano Science and Technology Institute, University of Science and Technology of China, 166 Ren Ai Road, Suzhou 215123, China.
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 IC50 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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