Design, synthesis, and biological evaluation of 2-amino-N-(2methoxyphenyl)-6-((4-nitrophenyl)sulfonyl)benzamide derivatives as potent HIV-1 Vif inhibitors

	Design, synthesis, and biological evaluation of 2-amino-N-(2methoxyphenyl)-6-((4-nitrophenyl)sulfonyl)benzamide derivatives as potent HIV-1 Vif inhibitors
	Zhang, RH; Wang, S; Luo, RH; Zhou, M; Zhang, H; Xu, GB; Zhao, YL; Li, YJ; Wang, YL; Yan, GY; Liao, SG; Zheng, YT; Li, R
	2019
发表期刊	BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN	0960-894X
卷号	29 期号:24
摘要	Viral infectivity factor (Vif) is one of the accessory protein of human immunodeficiency virus type I (HIV-1) that inhibits host defense factor, APOBEC3G (A3G), mediated viral cDNA hypermutations. Previous work developed a novel Vif inhibitor 2-amino-N-(2-methoxyphenyl)-6-((4-nitrophenyl)thio)benzamide (1) with strong antiviral activity. Through optimizations on the two side branches, a series of compound 1 derivatives (2-18) were designed, synthesized and tested in vitro for their antiviral activities. The biological results showed that compound 5 and 16 inhibited the virus replication efficiently with EC50 values of 9.81 and 4.62 mu M. Meanwhile, low cytotoxicities on H9 cells were observed for the generated compounds by the MTT assay. The structure-activity relationship of compound 1 was preliminarily clarified, which gave rise to the development of more potent Vif inhibitors.
收录类别	sci
语种	英语
文献类型	期刊论文
条目标识符	http://ir.kiz.ac.cn/handle/152453/13830
专题	科研部门_分子免疫药理学（郑永唐）
推荐引用方式 GB/T 7714	Zhang, RH,Wang, S,Luo, RH,et al. Design, synthesis, and biological evaluation of 2-amino-N-(2methoxyphenyl)-6-((4-nitrophenyl)sulfonyl)benzamide derivatives as potent HIV-1 Vif inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2019,29(24).
APA	Zhang, RH.,Wang, S.,Luo, RH.,Zhou, M.,Zhang, H.,...&Li, R.(2019).Design, synthesis, and biological evaluation of 2-amino-N-(2methoxyphenyl)-6-((4-nitrophenyl)sulfonyl)benzamide derivatives as potent HIV-1 Vif inhibitors.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,29(24).
MLA	Zhang, RH,et al."Design, synthesis, and biological evaluation of 2-amino-N-(2methoxyphenyl)-6-((4-nitrophenyl)sulfonyl)benzamide derivatives as potent HIV-1 Vif inhibitors".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 29.24(2019).

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