Synthesis and biological evaluation of water-soluble derivatives of chiral gossypol as HIV fusion inhibitors targeting gp41

被引：12

作者：

Yang, Jian ^{[1
]}

Li, Long-Long ^{[1
,3
]}

Li, Ju-Rong ^{[1
,3
]}

Yang, Jing-Xiang ^{[1
,3
]}

Zhang, Fang ^{[1
,3
]}

Chen, Gang ^{[1
,3
]}

Yu, Rui ^{[1
,3
]}

Ouyang, Wen-Jie ^{[2
]}

Wu, Shu-Wen ^{[2
]}

机构：

[1] Wuhan Univ, Dept Pharm, Renmin Hosp, Wuhan 430060, Hubei, Peoples R China

[2] Wuhan Univ, Coll Life Sci, Modern Virol Res Ctr, State Key Lab Virol, Wuhan 430072, Hubei, Peoples R China

[3] Wuhan Univ, Sch Pharmaceut Sci, Wuhan 430071, Hubei, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2018年 / 28卷 / 01期

基金：

中国国家自然科学基金;

关键词：

Chiral gossypol derivative; Amino acid derivative; D-Glucosamine derivative; Oligopeptide derivative; Taurine derivative; Anti-HIV-1; Gp41; IMMUNODEFICIENCY-VIRUS TYPE-1; ANTI-HIV-1; ACTIVITY; ENANTIOMER; PEPTIDE; ANALOGS; ENTRY;

D O I：

10.1016/j.bmcl.2017.08.049

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel or known water-soluble derivatives of chiral gossypol were synthesized and screened in vitro for their anti-HIV-1 activity. (-)-gossypol derivative was more active against HIV-1 than the corresponding (+)-gossypol derivative, respectively. Among these derivatives, D-glucosamine derivative of (-)-gossypol, oligopeptide derivative of (-)-gossypol and taurine derivative of (-)-gossypol, such as compounds 1a, 3a and 14a, showed significant inhibitory activities against HIV- 1 replication, HIV- 1-mediated cell- cell fusion and HIV gp41 6-helix bundle formation as some amino acid derivatives of (-)-gossypol. (C) 2017 Elsevier Ltd. All rights reserved.

引用

页码：49 / 52

页数：4

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