Design, Synthesis and Biological Evaluation of Caudatin Analogs as Potent Hepatitis B Virus Inhibitors

CORC > 昆明植物研究所 > 中国科学院昆明植物研究所 > 植物化学与西部植物资源持续利用国家重点实验室

	Design, Synthesis and Biological Evaluation of Caudatin Analogs as Potent Hepatitis B Virus Inhibitors
	Wang, Li-Jun 1; Chen, Hao 1,2; Ma, Yun-Bao 1; Huang, Xiao-Yan 1; Geng, Chang-An1 ; Zhang, Xue-Mei1 ; Chen, Ji-Jun1
刊名	MEDICINAL CHEMISTRY
	2015
卷号	11 期号:2 页码:165-179
关键词	Anti-HBV activity Caudatin analogs Hepatitis B e Antigen (HBeAg) Hepatitis B Surface Antigen (HBsAg) HBV DNA replication Structure-activity relationships(SARs) Synthesis
通讯作者	Chen,JJ (reprint author),Chinese Acad Sci,Kunming Inst Bot,State Key Lab Phytochem & Plant Resources West Ch,Kunming 650201,Peoples R China.
英文摘要	Thirty-nine caudatin analogs were designed and synthesized. Their anti-hepatitis B virus (HBV) activities were evaluated in vitro. Among them, twenty-three compounds showed much better anti-HBV activity than caudatin, and eleven compounds significantly inhibited the HBV DNA replication with IC50 values < 10 mu M. Interestingly, three compounds (22, 28, 29) exhibited excellent activity against the secretion of HBsAg (IC50 = 63.02 mu M, 52.81 mu M, 56.08 mu M), HBeAg (IC50 = 204.80 mu M, 173.51 mu M, 70.39 mu M), along with HBV DNA replication (IC50 = 24.55 mu M, 5.69 mu M, 8.23 mu M) with lower cytotoxicity. The structure-activity relationships (SARs) of these caudatin analogs were also discussed.
学科主题	Chemistry, Medicinal
类目[WOS]	Chemistry, Medicinal
研究领域[WOS]	Pharmacology & Pharmacy
关键词[WOS]	ANTI-HBV ; ACID-DERIVATIVES ; DRUG-RESISTANCE ; AGENTS ; REPLICATION ; ALISOL ; CELLS
收录类别	SCI
语种	英语
WOS记录号	WOS:000349331700008
内容类型	期刊论文
源URL	[http://ir.kib.ac.cn/handle/151853/20611]
专题	昆明植物研究所_植物化学与西部植物资源持续利用国家重点实验室
作者单位	1.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650201, Peoples R China 2.Chinese Acad Sci, Grad Univ, Beijing 100049, Peoples R China
推荐引用方式 GB/T 7714	Wang, Li-Jun,Chen, Hao,Ma, Yun-Bao,et al. Design, Synthesis and Biological Evaluation of Caudatin Analogs as Potent Hepatitis B Virus Inhibitors[J]. MEDICINAL CHEMISTRY,2015,11(2):165-179.
APA	Wang, Li-Jun.,Chen, Hao.,Ma, Yun-Bao.,Huang, Xiao-Yan.,Geng, Chang-An.,...&Chen, Ji-Jun.(2015).Design, Synthesis and Biological Evaluation of Caudatin Analogs as Potent Hepatitis B Virus Inhibitors.MEDICINAL CHEMISTRY,11(2),165-179.
MLA	Wang, Li-Jun,et al."Design, Synthesis and Biological Evaluation of Caudatin Analogs as Potent Hepatitis B Virus Inhibitors".MEDICINAL CHEMISTRY 11.2(2015):165-179.