Discovery of 5,6-Dihydro-indolo[1,2-a]quinoxaline Derivatives as New HIV-1 Inhibitors In Vitro

被引:28
作者
Fan, Ling-Ling [1 ]
Huang, Ning [2 ,3 ]
Yang, Rui-Ge [1 ]
He, Shu-Zhen [1 ]
Yang, Liu-Meng [2 ]
Xu, Hui [1 ]
Zheng, Yong-Tang [2 ]
机构
[1] NW A&F Univ, Coll Sci, Lab Pharmaceut Design & Synth, Yangling 712100, Peoples R China
[2] Chinese Acad Sci, Kunming Inst Zool, Key Lab Anim Models & Human Dis Mech, Chinese Acad Sci & Yunnan Prov, Kunming 650223, Yunnan, Peoples R China
[3] Chinese Acad Sci, Grad Sch, Beijing 100039, Peoples R China
关键词
5,6-Dihydro-indolo[1,2-a]quinoxaline; Acquired immunodeficiency syndrome; Human immunodeficiency virus-1; Inhibitor; AGENTS; ANALOGS;
D O I
10.2174/157018012798193026
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
In continuation of our program to find compounds with potent anti-human immunodeficiency virus type 1 (HIV-1) activities, seventeen 5,6-dihydro-indolo[1,2-a]quinoxaline derivatives (1-17) were preliminarily evaluated as HIV-1 inhibitors in vitro. Among all the derivatives, especially compounds 10 and 17 showed the most potent anti-HIV-1 activities with EC50 values of 2.42 and 3.39 mu g/mL, and TI values of 63.76 and 53.60, respectively.
引用
收藏
页码:44 / 47
页数:4
相关论文
共 15 条
[1]   New acyclic quinoxaline nucleosides. Synthesis and anti-HIV activity [J].
Ali, Ibrahim A. I. ;
Al-Masoudi, Iman A. ;
Aziz, Nazik M. ;
Al-Masoudi, Najim A. .
NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS, 2008, 27 (02) :146-156
[2]   Novel substituted quinoxaline 1,4-dioxides with in vitro antimycobacterial and anticandida activity [J].
Carta, A ;
Paglietti, G ;
Nikookar, MER ;
Sanna, P ;
Sechi, L ;
Zanetti, S .
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2002, 37 (05) :355-366
[3]   Synthesis and in vitro antitumor activity of new quinoxaline derivatives [J].
Corona, Paola ;
Carta, Antonio ;
Loriga, Mario ;
Vitale, Gabriella ;
Paglietti, Giuseppe .
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2009, 44 (04) :1579-1591
[4]   New developments in anti-HIV chemotherapy [J].
De Clercq, E .
BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR BASIS OF DISEASE, 2002, 1587 (2-3) :258-275
[5]   Anti HIV-1 Agents 2. Discovery of Dibenzofurans as New HIV-1 Inhibitors In Vitro [J].
Fan, Ling-Ling ;
Liu, Wu-Qing ;
Xu, Hui ;
Yang, Liu-Meng ;
Lv, Min ;
Zheng, Yong-Tang .
LETTERS IN DRUG DESIGN & DISCOVERY, 2009, 6 (03) :178-180
[6]   Synthesis and Anti-HIV-1 Activity of a Novel Series of Aminoimidazole Analogs [J].
Ganguly, Swastika ;
Murugesan, Sankaran ;
Prasanthi, Naru ;
Alpturk, Onur ;
Herman, Brian ;
Sluis-Cremer, Nicolas .
LETTERS IN DRUG DESIGN & DISCOVERY, 2010, 7 (05) :318-323
[7]   Anti HIV-1 Agents 7. Discovery of 1-Hydroxy-4-chloro-9,10-anthraquinone Derivatives as New HIV-1 Inhibitors in Vitro [J].
Huang, Ning ;
Wang, Qin ;
Yang, Liu-Meng ;
Xu, Hui ;
Zheng, Yong-Tang .
LETTERS IN DRUG DESIGN & DISCOVERY, 2011, 8 (07) :602-605
[8]   PRESENT STATUS AND FUTURE-PROSPECTS FOR HIV THERAPIES [J].
JOHNSTON, MI ;
HOTH, DF .
SCIENCE, 1993, 260 (5112) :1286-1293
[9]   Dipyridodiazepinone Analogs as Human Immunodeficiency Virus Type 1-Specific Non-Nucleoside Reverse Transcriptase Inhibitors: An Overview [J].
Lv, M. ;
Xu, H. .
CURRENT MEDICINAL CHEMISTRY, 2010, 17 (18) :1874-1898
[10]   The Quantitative Structure Activity Relationships for Predicting HIV Protease Inhibition by Substituted Fullerenes [J].
Martin, Dana ;
Karelson, Mati .
LETTERS IN DRUG DESIGN & DISCOVERY, 2010, 7 (08) :587-595