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

被引：5

作者：

Zhang, Rong-Hong ^{[2
,3
]}

Wang, Shan ^{[5
,7
]}

Luo, Rong-Hua ^{[4
]}

Zhou, Meng ^{[5
,7
]}

Zhang, Hong ^{[5
,7
]}

Xu, Guo-Bo ^{[5
,7
]}

Zhao, Yong-Long ^{[5
,7
]}

Li, Yong-Jun ^{[6
,7
]}

Wang, Yong-Lin ^{[6
,7
]}

Yan, Guoyi ^{[1
]}

Liao, Shang-Gao ^{[5
,7
]}

Zheng, Yong-Tang ^{[4
]}

Li, Rui ^{[1
]}

机构：

[1] Sichuan Univ, West China Hosp, State Key Lab Biotherapy, Chengdu 610041, Sichuan, Peoples R China

[2] Guizhou Med Univ, State Key Lab Funct & Applicat Med Plants & Tissu, Guiyang 550004, Guizhou, Peoples R China

[3] Guizhou Med Univ, Stem Cell Res Ctr, Guiyang 550004, Guizhou, Peoples R China

[4] Chinese Acad Sci, Kunming Inst Zool,Key Lab Bioact Peptides Yunnan, Ctr Biosafety Megasci,Key Lab Anim Models & Human, KIZ CUHK Joint Lab Bioresources & Mol Res Common, Kunming 650223, Yunnan, Peoples R China

[5] Guizhou Med Univ, Minist Educ, Engn Res Ctr Dev & Applicat Ethn Med & TCM, Guiyang, Guizhou, Peoples R China

[6] Guizhou Med Univ, Guizhou Prov Key Lab Pharmaceut, Guiyang, Guizhou, Peoples R China

[7] Guizhou Med Univ, Sch Pharm, Guian New Dist, Guizhou, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2019年 / 29卷 / 24期

基金：

中国国家自然科学基金;

关键词：

Vif inhibitors; Antiviral activity; Molecular docking; Structure-activity relationship; Optimization; SMALL-MOLECULE INHIBITION; APOBEC3G; REPLICATION; RESISTANCE;

D O I：

10.1016/j.bmcl.2019.126638

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

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.

引用

页数：4

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