Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR

[Display omitted] 30 new analogues of diarylpyrimidines were synthesized for further structural modifications, involving not only the linker but also the wing α of DAPYs. The anti-HIV-1 activities of all target molecules were evaluated, and most of them exhibited potent anti-HIV-1 (WT) activities an...

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Published in:Bioorganic & medicinal chemistry 2017-04, Vol.25 (8), p.2491-2497
Main Authors: Lu, Huan-Huan, Xue, Ping, Zhu, Yuan-Yuan, Ju, Xiu-Lian, Zheng, Xiao-Jiao, Zhang, Xun, Xiao, Ting, Pannecouque, Christophe, Li, Ting-Ting, Gu, Shuang-Xi
Format: Article
Language:English
Subjects:
AIDS
Anti-HIV
Anti-HIV Agents - pharmacology
Carbon-13 Magnetic Resonance Spectroscopy
Diarylpyrimidines
HIV-1 - drug effects
Molecular Docking Simulation
Nonnucleoside reverse transcriptase inhibitors
Proton Magnetic Resonance Spectroscopy
Pyrimidines - chemistry
Pyrimidines - pharmacology
Reverse Transcriptase Inhibitors - pharmacology
SAR
Spectrometry, Mass, Electrospray Ionization
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Summary:[Display omitted] 30 new analogues of diarylpyrimidines were synthesized for further structural modifications, involving not only the linker but also the wing α of DAPYs. The anti-HIV-1 activities of all target molecules were evaluated, and most of them exhibited potent anti-HIV-1 (WT) activities and low cytotoxicities. Among which, compound 4g showed excellent activities against WT HIV-1 with an EC50 value of 5.8nM and SI of up to 26,034. Another compound 4ab bearing a novel pyridinyl Wing α also displayed attractive activities. The structure-activity relationship (SAR) study was also summarized.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2017.03.009