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Indolizine Derivatives as HIV‐1 VIF–ElonginC Interaction Inhibitors |
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| Authors: | Wenlin Huang Tao Zuo Xiao Luo Hongwei Jin Zhenming Liu Zhenjun Yang Xianghui Yu Liangren Zhang Lihe Zhang |
| Institution: | 1. State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, , Beijing, 100191 China;2. National Engineering Laboratory for AIDS Vaccine, College of Life Science, Jilin University, , Changchun, 130012 China;3. Key Laboratory for Molecular Enzymology and Engineering of the Ministry of Education, College of Life Science, Jilin University, , Changchun, 130012 China |
| Abstract: | Compound 1 (VEC‐5) was identified as a potent small‐molecular HIV‐1 viron infectivity factor inhibitor that targets the viron infectivity factor–ElonginC interaction. A structure–activity relationship study was carried out to develop compounds with improved efficacy against HIV‐1 and 49 indolizine derivatives of three categories were designed and synthesized. We found that five compounds exhibited promising anti‐HIV‐1 activity, and the most active compound 2g had an IC50 value of 11.0 μm . These results provide new information to develop highly potent small‐molecule HIV‐1 viron infectivity factor inhibitors. |
| Keywords: | anti‐HIV‐1 indolizine derivatives structure– activity relationship VEC‐5 VIF– ElonginC interaction inhibition |