| Literature DB >> 28314514 |
Huan-Huan Lu1, Ping Xue1, Yuan-Yuan Zhu2, Xiu-Lian Ju1, Xiao-Jiao Zheng1, Xun Zhang1, Ting Xiao1, Christophe Pannecouque3, Ting-Ting Li4, Shuang-Xi Gu5.
Abstract
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.Entities:
Keywords: AIDS; Anti-HIV; Diarylpyrimidines; Nonnucleoside reverse transcriptase inhibitors; SAR
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Year: 2017 PMID： 28314514 DOI： 10.1016/j.bmc.2017.03.009
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641