Anti HIV-1 Agents 7. Discovery of 1-Hydroxy-4-chloro-9,10-anthraquinone Derivatives as New HIV-1 Inhibitors in Vitro

被引：4

作者：

Huang, Ning ^{[2
,3
]}

Wang, Qin ^{[1
]}

Yang, Liu-Meng ^{[2
]}

Xu, Hui ^{[1
]}

Zheng, Yong-Tang ^{[1
,2
]}

机构：

[1] NW A&F Univ, Lab Pharmaceut Design & Synth, Coll Sci, Yangling 712100, Peoples R China

[2] Chinese Acad Sci, Kunming Inst Zool, Chinese Acad Sci & Yunnan Prov, Key Lab Anim Models & Human Dis Mech, Kunming 650223, Yunnan, Peoples R China

[3] Chinese Acad Sci, Grad Sch, Beijing 100039, Peoples R China

来源：

LETTERS IN DRUG DESIGN & DISCOVERY | 2011年 / 8卷 / 07期

关键词：

1-Hydroxy-4-chloro-9,10-anthraquinone; Acquired immunodeficiency syndrome; Human immunodeficiency virus-1; Inhibitor; ANALOGS; ETHERS;

D O I：

10.2174/157018011796235185

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In continuation of our program aimed at the discovery and development of anti-HIV-1 agents, six 1-hydroxy-4-chloro-9, 10-anthraquinone derivatives (3-8) were prepared and preliminarily evaluated as HIV-1 inhibitors in vitro for the first time. Compounds 4 and 6 exhibited the potent anti-HIV-1 activities with EC(50) values of 9.81 and 17.90 mu g/mL, and TI values of >13.58 and >11.17, respectively. It demonstrated that introduction of the alkylacyloxy or alkylsulfonyloxy group at the 1-position of 1-hydroxy-4-chloro-9,10-anthraquinone could afford the more promising and potent compound than that having arylacyloxy or arylsulfonyloxy one.

引用

页码：602 / 605

页数：4

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