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Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR
Lu, Huan-Huan1; Xue, Ping1; Zhu, Yuan-Yuan2; Ju, Xiu-Lian1; Zheng, Xiao-Jiao1; Zhang, Xun1; Xiao, Ting1; Pannecouque, Christophe3; Li, Ting-Ting4; Gu, Shuang-Xi1
2017-04-15
Source PublicationBIOORGANIC & MEDICINAL CHEMISTRY
ISSN0968-0896
Volume25Issue:8Pages:2491-2497
Abstract30 new analogues of diarylpyrimidines were synthesized for further structural modifications, involving not only the linker but also the wing alpha of DAPYs. The anti-HIV-1 activities of all target molecules were evaluated, and most of them exhibited potent anti-HIV-1 (WT) activities and low cytotoxicities. Among which, compound 4g showed excellent activities against WT HIV-1 with an EC50 value of 5.8 nM and SI of up to 26,034. Another compound 4ab bearing a novel pyridinyl Wing a also displayed attractive activities. The structure-activity relationship (SAR) study was also summarized. (C) 2017 Elsevier Ltd. All rights reserved.
SubtypeArticle
KeywordAids Anti-hiv Diarylpyrimidines Nonnucleoside Reverse Transcriptase Inhibitors Sar
DOI10.1016/j.bmc.2017.03.009
WOS HeadingsScience & Technology ; Life Sciences & Biomedicine ; Physical Sciences
Indexed BySCI
Funding OrganizationNational Natural Science Foundation of China(21402148 ; National Natural Science Foundation of China(21402148 ; Hubei Provincial Department of Education of China(XD2014154) ; Hubei Provincial Department of Education of China(XD2014154) ; Wuhan Institute of Technology Scientific Research Fund(K201441 ; Wuhan Institute of Technology Scientific Research Fund(K201441 ; Wuhan Institute of Technology Teaching Research Project(X2015014) ; Wuhan Institute of Technology Teaching Research Project(X2015014) ; Wuhan Institute of Technology President Fund(2016079) ; Wuhan Institute of Technology President Fund(2016079) ; 21602164) ; 21602164) ; K201304) ; K201304) ; National Natural Science Foundation of China(21402148 ; National Natural Science Foundation of China(21402148 ; Hubei Provincial Department of Education of China(XD2014154) ; Hubei Provincial Department of Education of China(XD2014154) ; Wuhan Institute of Technology Scientific Research Fund(K201441 ; Wuhan Institute of Technology Scientific Research Fund(K201441 ; Wuhan Institute of Technology Teaching Research Project(X2015014) ; Wuhan Institute of Technology Teaching Research Project(X2015014) ; Wuhan Institute of Technology President Fund(2016079) ; Wuhan Institute of Technology President Fund(2016079) ; 21602164) ; 21602164) ; K201304) ; K201304)
Language英语
WOS Research AreaBiochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry
WOS SubjectBiochemistry & Molecular Biology ; Chemistry, Medicinal ; Chemistry, Organic
WOS KeywordREVERSE-TRANSCRIPTASE INHIBITORS ; PROTEIN-BINDING SITES ; MEDICINAL CHEMISTRY ; COLORIMETRIC ASSAY ; MOLECULAR DOCKING ; DRUG ; DESIGN ; SEARCH ; OPTIMIZATION ; RILPIVIRINE
WOS IDWOS:000399437100019
Funding OrganizationNational Natural Science Foundation of China(21402148 ; National Natural Science Foundation of China(21402148 ; Hubei Provincial Department of Education of China(XD2014154) ; Hubei Provincial Department of Education of China(XD2014154) ; Wuhan Institute of Technology Scientific Research Fund(K201441 ; Wuhan Institute of Technology Scientific Research Fund(K201441 ; Wuhan Institute of Technology Teaching Research Project(X2015014) ; Wuhan Institute of Technology Teaching Research Project(X2015014) ; Wuhan Institute of Technology President Fund(2016079) ; Wuhan Institute of Technology President Fund(2016079) ; 21602164) ; 21602164) ; K201304) ; K201304) ; National Natural Science Foundation of China(21402148 ; National Natural Science Foundation of China(21402148 ; Hubei Provincial Department of Education of China(XD2014154) ; Hubei Provincial Department of Education of China(XD2014154) ; Wuhan Institute of Technology Scientific Research Fund(K201441 ; Wuhan Institute of Technology Scientific Research Fund(K201441 ; Wuhan Institute of Technology Teaching Research Project(X2015014) ; Wuhan Institute of Technology Teaching Research Project(X2015014) ; Wuhan Institute of Technology President Fund(2016079) ; Wuhan Institute of Technology President Fund(2016079) ; 21602164) ; 21602164) ; K201304) ; K201304)
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Cited Times:8[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://ir.ihb.ac.cn/handle/342005/29181
Collection其他
Affiliation1.Wuhan Inst Technol, Sch Chem Engn & Pharm, Minist Educ, Key Lab Green Chem Proc, Wuhan 430205, Peoples R China
2.Wuhan Inst Technol, Sch Chem & Environm Engn, Wuhan 430205, Peoples R China
3.Katholieke Univ Leuven, Dept Microbiol & Immunol, Lab Virol & Chemotherapy, Rega Inst Med Res, B-3000 Leuven, Belgium
4.Chinese Acad Sci, Inst Hydrobiol, Wuhan 430072, Peoples R China
Recommended Citation
GB/T 7714
Lu, Huan-Huan,Xue, Ping,Zhu, Yuan-Yuan,et al. Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2017,25(8):2491-2497.
APA Lu, Huan-Huan.,Xue, Ping.,Zhu, Yuan-Yuan.,Ju, Xiu-Lian.,Zheng, Xiao-Jiao.,...&Gu, Shuang-Xi.(2017).Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR.BIOORGANIC & MEDICINAL CHEMISTRY,25(8),2491-2497.
MLA Lu, Huan-Huan,et al."Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR".BIOORGANIC & MEDICINAL CHEMISTRY 25.8(2017):2491-2497.
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