title: Panaxadiol and panaxatriol derivatives as anti-hepatitis B virus inhibitors.
abstract: 28 Derivatives of panaxadiol (PD) and panaxatriol were synthesized and evaluated for their anti-HBV activity on HepG 2.2.15 cells, of which 17 derivatives inhibited HBV DNA replication. Compounds 4, 9, 10, 14, and 15 showed moderate activity against HBV DNA replication with IC50 values ranged from 7.27 to 28.21 μM compared with PD. In particular, 3-O-2'-thenoyl panaxadiol (4) inhibited not only HBV DNA replication (IC50 = 16.5 μM, SI > 115.7) but also HBsAg (IC50 = 30.8 μM, SI > 62.0) and HBeAg (IC50 = 18.2 μM, SI > 105.14) secretions. Their structure-activity relationships were discussed for guiding future research toward the discovery of new anti-HBV agents.
authors: State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming, 650201 People's Republic of China ; University of Chinese Academy of Sciences, Beijing, 100049 People's Republic of China.
authors: Hao
authors: H
authors: Chen
authors: State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming, 650201 People's Republic of China.
authors: Li-Jun
authors: LJ
authors: Wang
authors: State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming, 650201 People's Republic of China.
authors: Yun-Bao
authors: YB
authors: Ma
authors: State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming, 650201 People's Republic of China.
authors: Xiao-Yan
authors: XY
authors: Huang
authors: State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming, 650201 People's Republic of China.
authors: Chang-An
authors: CA
authors: Geng
authors: State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming, 650201 People's Republic of China.
authors: Xue-Mei
authors: XM
authors: Zhang
authors: State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming, 650201 People's Republic of China.
authors: Ji-Jun
authors: JJ
authors: Chen
keywords: Anti-HBV activity; Chemical modification; Panaxadiol and panaxatriol derivatives; Structure–activity relationships