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Design and synthesis of novel nitrogen-containing polyhydroxylated aromatics as HIV-1 integrase inhibitors from caffeic acid phenethyl ester |
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| Authors: | Peng Wang Chuan Liu Tino Sanches Yuan Zhong Bo Liu Junlong Xiong Nouri Neamati Guisen Zhao |
| Affiliation: | 1. School of Pharmaceutical Sciences, Shandong University, Ji’nan, Shandong Province 250012, PR China;2. Department of Pharmaceutical Sciences, School of Pharmacy, University of Southern California, Los Angeles, CA 90089, USA |
| Abstract: | A series of nitrogen-containing polyhydroxylated aromatics from caffeic acid phenethyl ester were designed and synthesized as HIV-1 integrase inhibitors. Most of these compounds exhibited potent inhibitory activities at micromolar concentrations against HIV-1 integrase in the 3′-end processing and the strand transfer. Their key structure–activity relationship was also discussed. |
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