Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR

doi:10.1016/j.bmc.2017.03.009

CORC > 水生生物研究所 > 中科院水生所知识产出（2009年前） > 其他 > 期刊论文

	Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR
	Lu, Huan-Huan 1; Xue, Ping 1; Zhu, Yuan-Yuan 2; Ju, Xiu-Lian 1; Zheng, Xiao-Jiao 1; Zhang, Xun 1; Xiao, Ting 1; Pannecouque, Christophe 3; Li, Ting-Ting 4; Gu, Shuang-Xi 1
刊名	BIOORGANIC & MEDICINAL CHEMISTRY
	2017-04-15
卷号	25 期号:8 页码:2491-2497
关键词	AIDS Anti-HIV Diarylpyrimidines Nonnucleoside reverse transcriptase inhibitors SAR
ISSN号	0968-0896
DOI	10.1016/j.bmc.2017.03.009
英文摘要	30 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.
资助项目	National Natural Science Foundation of China[21402148] ; National Natural Science Foundation of China[21602164] ; Hubei Provincial Department of Education of China[XD2014154] ; Wuhan Institute of Technology Scientific Research Fund[K201441] ; Wuhan Institute of Technology Scientific Research Fund[K201304] ; Wuhan Institute of Technology Teaching Research Project[X2015014] ; Wuhan Institute of Technology President Fund[2016079]
WOS关键词	REVERSE-TRANSCRIPTASE INHIBITORS ; PROTEIN-BINDING SITES ; MEDICINAL CHEMISTRY ; COLORIMETRIC ASSAY ; MOLECULAR DOCKING ; DRUG ; DESIGN ; SEARCH ; OPTIMIZATION ; RILPIVIRINE
WOS研究方向	Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry
语种	英语
出版者	PERGAMON-ELSEVIER SCIENCE LTD
WOS记录号	WOS:000399437100019
资助机构	National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; National Natural Science Foundation of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Hubei Provincial Department of Education of China ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Scientific Research Fund ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology Teaching Research Project ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund ; Wuhan Institute of Technology President Fund
内容类型	期刊论文
源URL	[http://ir.ihb.ac.cn/handle/342005/32616]
专题	水生生物研究所_其他_期刊论文
通讯作者	Zhu, Yuan-Yuan; Pannecouque, Christophe; Gu, Shuang-Xi
作者单位	1.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
推荐引用方式 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.