Synthesis and HIV-1 integrase inhibition activity of some N-arylindoles.
Eight simple N-arylindoles were designed, synthesized and evaluated as human immunodeficiency virus (HIV)-1 integrase inhibitors in vitro for the first time. Among these compounds, 3b, 3e and 3g demonstrated significant anti-HIV-1 integrase activity. Especially 3b showed the highest anti-HIV-1 integrase activity with EC50 value of 7.88 microg/ml and TI value of 24.61. Meantime, some structure-activity relationships were also observed and will provide a new lead for design and discovery of more potent N-arylindoles as HIV-1 integrase inhibitors.
Xu
Hui
H
Laboratory of Pharmaceutical Synthesis, College of Sciences, Northwest A&F University, Yangling, China. orgxuhui@nwsuaf.edu.cn
Liu
Wu-Qing
WQ
Fan
Ling-Ling
LL
Chen
Yang
Y
Yang
Liu-Meng
LM
Lv
Lei
L
Zheng
Yong-Tang
YT
D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D002855:Chromatography, Thin Layer; D015726:Giant Cells / Q000187:drug effects; D019428:HIV Integrase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D015497:HIV-1 / Q000187:drug effects / Q000201:enzymology; D006801:Humans; D007202:Indicators and Reagents; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D013329:Structure-Activity Relationship; D013778:Tetrazolium Salts; D013844:Thiazoles
D019428:HIV Integrase Inhibitors; D007202:Indicators and Reagents; D007211:Indoles; D013778:Tetrazolium Salts; D013844:Thiazoles; C022616:thiazolyl blue