Design, synthesis, and molecular hybrids of caudatin and cinnamic acids as novel anti-hepatitis B virus agents

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 molecular hybrids of caudatin and cinnamic acids as novel anti-hepatitis B virus agents
	Wang, Li-Jun 1,2; Geng, Chang-An1 ; Ma, Yun-Bao 1; Luo, Jie 1; Huang, Xiao-Yan 1; Chen, Hao 1,2; Zhou, Ning-Jia 1,2; Zhang, Xue-Mei1 ; Chen, Ji-Jun1
刊名	EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
	2012-08-01
卷号	54 页码:352-365
关键词	Synthesis Molecular hybrids Caudatin derivatives Anti-hepatitis B virus Unique mechanisms
ISSN号	0223-5234
通讯作者	Chen, JJ (reprint author), Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources W China, 132 Lanhei Rd, Heilongtan 650201, Kunming, Peoples R China.,chenjj@mail.kib.ac.cn
英文摘要	Forty-six conjugated derivatives of caudatin with substituted cinnamic acids were synthesized, and their anti-hepatitis B virus (HBV) activity was evaluated in HepG 2.2.15 cells. Most of the derivatives exhibited potent anti-HBV activity, especially inhibiting the HBV DNA replication with the IC50 values from 2.44 to 22.89 mu M. Compound 18 showed significant activity against the secretion of HBsAg, HBeAg, and HBV DNA replication with IC50 values of 5.52, 5.52, 2.44 mu M, respectively, and had good safety (LD50 > 1250 mg/kg) according to the acute toxicity study. Preliminary mechanism investigation suggested that compound 18 exerted antivirus effects via interfering HBV X promoter and enhancer 1 to influence HBV transcriptions. (C) 2012 Elsevier Masson SAS. All rights reserved.
类目[WOS]	Chemistry, Medicinal
研究领域[WOS]	Pharmacology & Pharmacy
关键词[WOS]	GENE-EXPRESSION ; PREGENOMIC PROMOTER ; ANTIVIRAL ACTIVITY ; BINDING-PROTEIN ; IN-VITRO ; X-GENE ; DERIVATIVES ; HBV ; ENHANCER ; INHIBITORS
收录类别	SCI ; IC
资助信息	National Natural Science Foundation of China for Distinguished Young Scholars [81025023]
语种	英语
WOS记录号	WOS:000307920600037
公开日期	2012-11-30
内容类型	期刊论文
源URL	[http://ir.kib.ac.cn/handle/151853/15720]
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 W China, Heilongtan 650201, Kunming, 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,Geng, Chang-An,Ma, Yun-Bao,et al. Design, synthesis, and molecular hybrids of caudatin and cinnamic acids as novel anti-hepatitis B virus agents[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2012,54:352-365.
APA	Wang, Li-Jun.,Geng, Chang-An.,Ma, Yun-Bao.,Luo, Jie.,Huang, Xiao-Yan.,...&Chen, Ji-Jun.(2012).Design, synthesis, and molecular hybrids of caudatin and cinnamic acids as novel anti-hepatitis B virus agents.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,54,352-365.
MLA	Wang, Li-Jun,et al."Design, synthesis, and molecular hybrids of caudatin and cinnamic acids as novel anti-hepatitis B virus agents".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 54(2012):352-365.