| C15-Imines of Natural Matrine Alkaloid as Anti-HIV-1 Agents |
| Lv, M; Huang, N; Li, JJ; Yang, LM; Zhang, SY; Ma, QJ; Zheng, YT; Xu, H
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| 2024
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| 发表期刊 | LETTERS IN DRUG DESIGN & DISCOVERY
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| ISSN | 1570-1808
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| 卷号 | 21期号:2页码:376-379 |
| 摘要 | Background: Human immunodeficiency virus (HIV) infection and acquired immunodeficiency syndrome (AIDS) have resulted in a global health threat. Meanwhile, due to the emergence of drug-resistant HIV-1 strains, the discovery of potent compounds for antiretroviral therapy success is highly desirable.Objective: This study aimed to develop anti-HIV-1 candidates which can be effectively applied for the treatment of HIV infection.Methods: Based upon our previous results, a series of E isomers of C15-imines of matrine (3a-l) were semi-synthesized from a natural quinolizidine alkaloid matrine. Their anti-HIV-1 activities were evaluated against HIV-1IIIB replication in acutely infected C8166 cells in vitro.Results: Derivatives 3c, 3h and 3j showed good anti-HIV-1 activities with EC50 and therapeutic index (TI) values of 0.0089/0.012/0.0091 mM, and 23.71/32.49/27.43, respectively.Conclusion: The substituents and their corresponding positions on the phenyl ring of C15-imine derivatives of matrine were vital for anti-HIV-1 activities. Compounds 3c, 3h and 3j can be used as leads for further structural modification as HIV-1 inhibitors. |
| 收录类别 | sci
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| 语种 | 英语
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| 文献类型 | 期刊论文
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| 条目标识符 | http://ir.kiz.ac.cn/handle/152453/14209
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| 专题 | 科研部门_分子免疫药理学（郑永唐）
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推荐引用方式
GB/T 7714 |
Lv, M,Huang, N,Li, JJ,et al. C15-Imines of Natural Matrine Alkaloid as Anti-HIV-1 Agents[J]. LETTERS IN DRUG DESIGN & DISCOVERY,2024,21(2):376-379.
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| APA |
Lv, M.,Huang, N.,Li, JJ.,Yang, LM.,Zhang, SY.,...&Xu, H.(2024).C15-Imines of Natural Matrine Alkaloid as Anti-HIV-1 Agents.LETTERS IN DRUG DESIGN & DISCOVERY,21(2),376-379.
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| MLA |
Lv, M,et al."C15-Imines of Natural Matrine Alkaloid as Anti-HIV-1 Agents".LETTERS IN DRUG DESIGN & DISCOVERY 21.2(2024):376-379.
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