Research
| Title： | Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR |
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| First author： | 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 |
| Journal： | BIOORGANIC & MEDICINAL CHEMISTRY |
| Years： | 2017 |
| DOI： | 10.1016/j.bmc.2017.03.009 |
| Abstract： | 30 new analogues of diarylpyrimidines were synthesized for further structural modifications, involving not only the linker but also the wing alpha 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 5.8 nM and SI of up to 26,034. Another compound 4ab bearing a novel pyridinyl Wing a also displayed attractive activities. The structure-activity relationship (SAR) study was also summarized. (C) 2017 Elsevier Ltd. All rights reserved. |
