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Design,synthesis and anti-hbv activity of novel bis(trifluoroethyl)phosphonomethyl ether derivatives of acyclovir

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Chinese Chemical Letters 2009年第5期20卷 507-510页

作者： Peng Lu Sai Hong Jiang Jiang Xia Liu Yu She Yang Ru Yun Ji State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Shanghai Institute for Biological Sciences Chinese Academy of Science Shanghai 201203 China Fudan University Shanghai 200032 China

A series of novel bis（trifluoroethyl）phosphonomethyl ether derivatives of acyclovir was synthesized and their in vitro anti-hbv activity was evaluated in HepG2 2.2.15 cells. In contrast to acyclovir, most of the described phosphonates emerged as potent inhibitors of hbv replication. Especially, the most active compound 11 with IC50 value of 2.92 μmol/L was 33 times more potent than acyclovir with ICso value of 100 μmol/L.

关键词： Acyclovir Phosphonate anti-hbv activity

Synthesis and anti-hbv activity of novel 5-substituted pyridin-2(1H)-one derivatives

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Chinese Chemical Letters 2010年第3期21卷 290-292页

作者： Zhang, Yi Kai Lv, Zhi Liang Niu, Chun Juan Li, Ke Second Mil Med Univ Dept Med Chem Sch Pharm Shanghai 200433 Peoples R China

Four novel 5-substituted pyridine-2(1H)-one derivatives were designed and synthesized by using addition–elimination reactions. The structures of these novelly synthesized compounds were verified by 1 H NMR, ESI-MS and single crystal X-ray diffraction. Furthermore, all four compounds (most notably compound 7a ) were found to be highly efficient against hepatitis B virus (hbv) in cultured HepG2 2.2.15 cell, making them promising drug candidates for potential bioactive molecule against hepatitis B.

关键词： 5-Substituted pyridin-2（1H）-one Synthesis Crystal structure anti-hbv activity

A new sesquiterpene lactone from the fruits of Illicium henryi

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Chinese Journal of Natural Medicines 2014年第6期12卷 477-480页

作者： LIU Ji-Feng LI Hui-Juan ZHANG Jing-Min WANG Li-Xia WANG Ya-Feng LIU Meng-Qi BI Yue-Feng ZHANG Yan-Bing School of Pharmaceutical Science Zhengzhou University Henan Key laboratory for Pharmacology of Liver Disease Academy of Medical and Pharmaceutical Science Zhengzhou University School of Pharmaceutical Science Henan University of Traditional Chinese Medicine

AIM: To study the chemical constituents of the fruits of Illicium henryi. METHOD: Chromatographic separations on silica gel, Sephadex LH-20 gel and MCI gel were used to isolate the compounds. The structures were elucidated based on extensive spectroscopic data analyses. RESULTS: Seven compounds were obtained and their structures were identified as 10-benzoyl-cycloparvifloralone(1), cycloparvifloralone(2), 2α-hydroxycycloparviforalone(3), henrylactone B(4), merrillianone(5), henrylactone C(6) and 7, 14-ortholactone-3-hydroxyfloridanolide(7). CONCLUSION: Compound 1 is a new sesquiterpene lactone. The tested compounds showed weak anti-hbv activities on hbv surface antigen(HBsAg) secretion and hbv e antigen(HBeAg) secretion using Hep G2.2.15 cell line.

关键词： Illicium henryi Sesquiterpene lactones anti-hbv activity

Sophaloseedlines A-G: Diverse Matrine-Based Alkaloids from Sophora alopecuroides with Potential anti-Hepatitis B Virus Activities

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Chinese Journal of Chemistry 2021年第9期39卷 2555-2562页

作者： Ding Luo Zhong-Nan Wu Ji-Hui Zhang Qiang Lin Neng-Hua Chen Si Chen Qing Tang Zhao-Chun Zhan Chun-Lin Fan Yao-Lan Li Guo-Cai Wang Yu-Bo Zhang Institute of Traditional Chinese Medicine&Natural Products Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs ResearchCollege of PharmacyJinan UniversityGuangzhouGuangdong 510632China Guangdong Clinical Translational Center for Targeted Drug Department of PharmacologySchool of MedicineJinan UniversityGuangzhouGuangdong 510632China

Sophaloseedlines A-G(1-7),seven new matrine-based alkaloids along with two known analogues,were isolated from the seeds of Sophora alopecuroides.The new structures were determined based on extensive spectroscopic data,electronic circular dichroism calculations,and X-ray crystallography.Notably,sophaloseedline A(1)represents a novel rearranged 6(5→17)-abeo-matrine alkaloid featuring unprecedented highly constructed 7/6/5/6 tetracyclic fused ring skeleton.The hypothetical biosynthetic pathways for sophaloseedli nes A-F were proposed based on co-existing precursors.Additionally,all the isolated alkaloids were screened for their antiviral activities against hepatitis B virus,and new alkaloids 1 and 2 displayed more potent activities than those of matrine(a parent alkaloid of title plant)and positive control(lamivudine).

关键词： Sophora alopecuroides Matrine-based alkaloid Structure elucidation anti-hbv activity Biological activity

The Progress of anti-hbv Constituents from Medicinal Plants in China

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Natural Products and Bioprospecting 2018年第4期8卷 227-244页

作者： Chang-An Geng Ji-Jun Chen State Key Laboratory of Phytochemistry and Plant Resources in West China Kunming Institute of BotanyChinese Academy of SciencesNo.132 Lanhei RoadKunming 650201China Yunnan Key Laboratory of Natural Medicinal Chemistry Kunming 650201China University of Chinese Academy of Sciences Beijing 100049China

Hepatitis B virus(hbv)infection causing acute and chronic hepatitis is a serious problem worldwide,whereas the current treatment methods are unsatisfactory.Traditional Chinese herbs that have long been used for medicinal purposes are fascinating sources for novel anti-hbv candidates.This paper summarizes the progress of anti-hbv constituents from diverse medicinal plants in China to provide information for searching new anti-hbv drugs from natural sources.

关键词： Hepatitis B virus anti-hbv activity Medicinal plants HBsAg HBeAg hbv DNA

Design, synthesis and in vitro evaluation of L-amino acid esters prodrugs of acyclic nucleoside phosphonates as anti-hbv agent

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Chinese Chemical Letters 2007年第7期18卷 817-819页

作者： Xiao Zhong Fu Sai Hong Jiang Jian Xin Yu She Yang RU Yun Ji School of Pharmacy Guiyang Medical College Guiyang 550004 China State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Shanghai Institute for Biological SciencesChinese Academy of Science Shanghai 201203 China Shanghai Fudan-Yueda Bio-Tech Co. Ltd. Shanghai 201203 China

A series of novel L-amino acid esters prodrugs of acyclic nucleoside phosphonates was synthesized and their anti-hbv activity was evaluated in HepG2 2.2.15 cells. Compound 1d exhibited more potent anti-hbv activity and lower cytotoxicity than those of adefovir dipivoxil with EC50 and CC50 values of 0.207 μmol/L and 2530 μmol/L, respectively.

关键词： Acyclic nucleoside phosphonates L-Amino acid Prodrug anti-hbv activity

Synthesis and in vitro anti-hepatitis B virus activity of 1H-benzimidazol-5-ol derivatives

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Chinese Chemical Letters 2010年第11期21卷 1326-1329页

作者： Dong Chen Xin Zhai Qiu Hui Yuan Jian Luo Si Chang Xie Ping Gong Key Laboratory of Original New Drugs Design and Discovery of Ministry of Education School of Pharmaceutical EngineeringShenyang Pharmaceutical UniversityShenyang 110016China

A series of 1H-benzimidazol-5-ol derivatives were synthesized and evaluated for their anti-hepatitis B virus(hbv) activity and cytotoxicity in HepG2.2.15 cells.Half of the tested compounds were found to be potent against HBsAg secretion with IC50 values less than 100μmol/L.Compounds 14c,14d,and 14e showed significant inhibitory activity to the viral antigen HBeAg.

关键词： 1H-benzimidazol-5-ol Synthesis anti-hbv activity

Panaxadiol and Panaxatriol Derivatives as anti-Hepatitis B Virus Inhibitors

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Natural Products and Bioprospecting 2014年第3期4卷 163-174页

作者： Hao Chen Li-Jun Wang Yun-Bao Ma Xiao-Yan Huang Chang-An Geng Xue-Mei Zhang Ji-Jun Chen State Key Laboratory of Phytochemistry and Plant Resources in West China Kunming Institute of BotanyChinese Academy of SciencesKunming 650201People’s Republic of China University of Chinese Academy of Sciences Beijing 100049People’s Republic of China

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.

关键词： Chemical modification Panaxadiol and panaxatriol derivatives anti-hbv activity Structure-activity relationships

Synthesis and Biological Evaluation of Entecavir 4＇-Ester Derivatives

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Chemical Research in Chinese Universities 2014年第5期30卷 749-754页

作者： FENG Deri LIU Jiaan LIANG Shuang WANG Yanyan XU Youjun School of Pharmaceutical Engineering Shenyang Pharmaceutical University Shenyang 110016 P. R. China

Entecavir can significantly inhibit the replication of hbv-DNA, reduce the hbv-DNA level in blood se- rum. But suffering from low oral bioavailability, entecavir has low intestinal membrane permeability and poor meta- bolic stability. In this study, 12 different derivatives of entecavir 4＇-ester were regioselectively synthesized and their apical-to-basolateral permeabilities across Caco-2 cells and hbv-DNA inhibitory efficacies were evaluated. Most of the compounds showed high permeabilities across Caco-2 cells compared with entecavir, compounds 5b and 5e also exhibited comparable anti-hbv activities with that of entecavir, especially.

关键词： Entecavir anti-hbv activity Intestinal membrane permeability