Discovery of novel paeonol-based derivatives against skin inflammation in vitro and in vivo

Jing Wu, Ren De Zhu, Guo Min Cao, Jun Cheng Du, Xin Liu, Liang Zhuo Diao, Zhao Yan Zhang, Yang Sheng Hu, Xin Hua Liu & Jing Bo Shi
T-LAK-cell-originated protein kinase (TOPK), a novel member of the mitogen-activated protein kinase family, is considered an effective therapeutic target for skin inflammation. In this study, a series (A − D) of paeonol derivatives was designed and synthesised using a fragment growing approach, and their anti-inflammatory activities against lipopolysaccharide (LPS)-induced nitric oxide production in RAW264.7 cells were tested. Among them, compound B12 yielded the best results (IC50 = 2.14 μM) with low toxicity (IC50 > 50...
1 citation reported since publication in 2022.
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