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Terpenoids. III: Synthesis and biological evaluation of 23-hydroxybetulinic acid derivatives as novel inhibitors of glycogen phosphorylase |
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| Authors: | Peiqing Zhu Yi Bi Jinyi Xu Zan Li Jun Liu Luyong Zhang Wencai Ye Xiaoming Wu |
| Affiliation: | 1. Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tongjia Xiang, Nanjing, Jiangsu 210009, China;2. Center for Drug Discovery, China Pharmaceutical University, 1 Shennonglu, Nanjing 210038, China;3. Jiangsu Center for Drug Screening, China Pharmaceutical University, 1 Shennonglu, Nanjing 210038, China;4. Department of Phytochemistry, China Pharmaceutical University, 1 Shennonglu, Nanjing 210038, China |
| Abstract: | A series of 23-hydroxybetulinic acid derivatives were prepared and tested in vitro as a new class of inhibitors of glycogen phosphorylase (GP). Within this series of compounds, 12b (IC50 = 3.5 μM) is the most potent GPa inhibitor. The preliminary SAR results of the 23-hydroxybetulinic acid derivatives are discussed. |
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