Synthesis, structure–activity relationships and biological evaluation of dehydroandrographolide and andrographolide derivatives as novel anti-hepatitis B virus agents

Dehydroandrographolide and andrographolide, two natural diterpenoids isolated from Andrographis paniculata possessed activity against HBV DNA replication with IC50 values of 22.58 and 54.07μM and low SI values of 8.7 and 3.7 in our random assay. Consequently, 48 derivatives of dehydroandrographolide...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2014-05, Vol.24 (10), p.2353-2359
Hauptverfasser:	Chen, Hao, Ma, Yun-Bao, Huang, Xiao-Yan, Geng, Chang-An, Zhao, Yong, Wang, Li-Jun, Guo, Rui-Hua, Liang, Wen-Juan, Zhang, Xue-Mei, Chen, Ji-Jun
Format:	Artikel
Sprache:	eng
Schlagworte:	Andrographis paniculata Anti-HBV activity Antiviral Agents - chemical synthesis Antiviral Agents - chemistry Antiviral Agents - pharmacology Biological Products Dehydroandrographolide and andrographolide derivatives Diterpenes - chemical synthesis Diterpenes - chemistry Diterpenes - pharmacology DNA Replication - drug effects DNA, Viral - biosynthesis DNA, Viral - genetics Hepatitis B virus Hepatitis B virus - drug effects Hepatitis B virus - genetics Hepatitis B virus - physiology Octanol–water partition coefficients Structure-Activity Relationship Structure–activity relationships Virus Replication - drug effects
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