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学科主题: 药学
题名:
Indolizine Derivatives as HIV-1 VIFElonginC Interaction Inhibitors
作者: Huang, Wenlin1; Zuo, Tao2; Luo, Xiao1; Jin, Hongwei1; Liu, Zhenming1; Yang, Zhenjun1; Yu, Xianghui2,3; Zhang, Liangren1; Zhang, Lihe1
关键词: anti-HIV-1 ; indolizine derivatives ; structureactivity relationship ; VEC-5 ; VIFElonginC interaction inhibition
刊名: CHEMICAL BIOLOGY & DRUG DESIGN
发表日期: 2013-06-01
DOI: 10.1111/cbdd.12119
卷: 81, 期:6, 页:730-741
收录类别: SCI ; IC
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Biochemistry & Molecular Biology ; Chemistry, Medicinal
研究领域[WOS]: Biochemistry & Molecular Biology ; Pharmacology & Pharmacy
关键词[WOS]: SMALL-MOLECULE INHIBITION ; 1,3-DIPOLAR CYCLOADDITION ; VIF PROTEINS ; YLIDES
英文摘要:

Compound 1 (VEC-5) was identified as a potent small-molecular HIV-1 viron infectivity factor inhibitor that targets the viron infectivity factorElonginC interaction. A structureactivity relationship study was carried out to develop compounds with improved efficacy against HIV-1 and 49 indolizine derivatives of three categories were designed and synthesized. We found that five compounds exhibited promising anti-HIV-1 activity, and the most active compound 2g had an IC50 value of 11.0m. These results provide new information to develop highly potent small-molecule HIV-1 viron infectivity factor inhibitors.

语种: 英语
所属项目编号: 20972009 ; 20090001120049
项目资助者: National Natural Science Foundation of China ; Ministry of Education of China
WOS记录号: WOS:000319417100006
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/58350
Appears in Collections:北京大学药学院_期刊论文

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作者单位: 1.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
2.Jilin Univ, Coll Life Sci, Natl Engn Lab AIDS Vaccine, Changchun 130012, Peoples R China
3.Jilin Univ, Coll Life Sci, Minist Educ, Key Lab Mol Enzymol & Engn, Changchun 130012, Peoples R China

Recommended Citation:
Huang, Wenlin,Zuo, Tao,Luo, Xiao,et al. Indolizine Derivatives as HIV-1 VIFElonginC Interaction Inhibitors[J]. CHEMICAL BIOLOGY & DRUG DESIGN,2013,81(6):730-741.
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