| 论文摘要： |
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. |
