Synthesis and anti-HIV activity of 2-naphthyl substituted DAPY analogues as non-nucleoside reverse transcriptase inhibitors

被引：37
|
作者：
Liang, Yong-Hong [1 ]
He, Qiu-Qin [1 ]
Zeng, Zhao-Sen [1 ]
Liu, Zhi-Qian [1 ]
Feng, Xiao-Qing [1 ]
Chen, Fen-Er [1 ,2 ]
Balzarini, Jan [3 ]
Pannecouque, Christophe [3 ]
De Clercq, Erik [3 ]
机构：
[1] Fudan Univ, Dept Chem, Shanghai 200433, Peoples R China
[2] Fudan Univ, Inst Biomed Sci, Shanghai 200433, Peoples R China
[3] Katholieke Univ Leuven, Rega Inst Med Res, B-3000 Louvain, Belgium
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2010年 / 18卷 / 13期
基金：
中国国家自然科学基金;
关键词：
HIV-1; Reverse transcriptase; NNRTIs; DAPY; DIARYLPYRIMIDINE ANALOGS; COLORIMETRIC ASSAY; ANTIVIRAL ACTIVITY; MUTANT STRAINS; WILD-TYPE;
D O I：
10.1016/j.bmc.2010.05.036
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
Nine newly 6-cynao-2-naphthyl substituted diarylpyrimidines (DAPY) were synthesized as non-nucleoside reverse transcriptase inhibitors on the basis of our previous work. The antiviral and cytotoxicity evaluation indicated that these compounds displayed strong activity against wild-type HIV-1 at nanomolar concentrations with selectivity index SI greater than 23 779. The most active compounds 3c and 3e exhibited activity against the double mutant (103N+181C) strains at an EC50 of 0.16 and 0.15 mu M, and were more activity than that of efavirenz. (C) 2010 Elsevier Ltd. All rights reserved.
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页码：4601 / 4605
页数：5
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