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Synthesis and Biological Evaluation of Strictosamide Derivatives with Improved Antiviral and Antiproliferative Activities |
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| Authors: | Zan Li Zhaoliang Li Yunwei Lin Zhaoqing Meng Gang Ding Liang Cao Na Li Wenjun Liu Wei Xiao Xiaoming Wu Jinyi Xu |
| Institution: | 1. State Key Laboratory of Natural Medicines and Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing, China;2. Jiangsu Zeukov Pharmaceutical S&T. Inc, Jiangsu, Nanjing, China;3. State Key Lab of New‐tech for Chinese Medicine Pharmaceutical Process, Jiangsu, Lianyungang, China |
| Abstract: | A series of novel derivatives of strictosamide were synthesized and biologically evaluated. Most of the new compounds exhibited improved activities than the parent compound strictosamide. Among them, compounds Ib and If possessed antiviral activities against influenza A virus (A/Jinan/15/90) with IC50 values of 4.12 and 12.35 μg/mL, respectively. Compound Ie possessed antiviral activity against respiratory syncytial virus (RSV) with an IC50 value of 9.58 μg/mL. Both compounds IIc and IId had moderate antiproliferative effects against five human cancer cell lines. The preliminary structure‐activity relationships were also concluded. This study provides a promising new template with potential antiviral activity. |
| Keywords: | antiproliferative effect antiviral activity derivatives SARs strictosamide |