Synthesis of hemslecin A derivatives: A new class of hepatitis B virus inhibitors |
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Authors: | Rui-Hua Guo Chang-An Geng Xiao-Yan Huang Yun-Bao Ma Quan Zhang Li-Jun Wang Xue-Mei Zhang Rong-Ping Zhang Ji-Jun Chen |
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Institution: | 1. State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650204, PR China;2. Kunming Medical University, Kunming, Yunnan 650500, PR China |
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Abstract: | A series of hemslecin A derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activities, namely, inhibiting the secretion of hepatitis B surface antigen (HBsAg), hepatitis B e antigen (HBeAg), and HBV DNA replication on HepG 2.2.15 cells. Most of the derivatives showed enhanced anti-HBV activities, of which compounds A1–A7, B5, C and E exhibited significant activities inhibiting HBV DNA replication with IC50 values of 2.8–11.6 μM, comparable to that of the positive control, tenofovir. Compounds A1–A3, A5, B5, and C displayed low cytotoxicities, which resulted in high SI values of 89.7, 55.6, 77.8, >83.4, >55.8, and >150.5, respectively. |
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