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Panaxadiol and panaxatriol derivatives as anti-hepatitis B virus inhibitors (from Nat. Prod. Bioprospect, 2016, 4, 163-174)
Bibliografi
Author:
Chen, Hao
;
Wang, Li-Jun
;
Ma, Yun-Bao
;
Huang, Xiao-Yan
;
Geng, Chang-An
;
Zhang, Xue-mei
;
Chen, Ji-Jun
Topik:
Chemical modification
;
Panaxadiol and panaxatriol derivatives
;
Anti-HBV activity
;
Structure–activity relationships
;
Hepatitis - Drug
Bahasa:
(EN )
Penerbit:
The Author(s)
Tahun Terbit:
2014
Jenis:
Article - diterbitkan di jurnal ilmiah internasional
Fulltext:
art_3A10.1007_2Fs13659-014-0018-2.pdf
(1.85MB;
0 download
)
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 lM compared with PD. In particular, 3-O-20-thenoyl panaxadiol (4) inhibited not only HBV DNA replication (IC50 = 16.5 lM, SI[115.7) but also HBsAg (IC50 = 30.8 lM, SI [62.0) and HBeAg (IC50 = 18.2 lM, SI [105.14) secretions. Their structure–activity relationships were discussed for guiding future research toward the discovery of new anti-HBV agents.
[hepatitis - drug]
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