Indolizine Derivatives as HIV‐1 VIF–ElonginC Interaction Inhibitors
Chemical Biology & Drug Design2013Vol. 81(6), pp. 730–741
Citations Over TimeTop 12% of 2013 papers
Wenlin Huang, Tao Zuo, Xiao Luo, Hongwei Jin, Zhenming Liu, Zhenjun Yang, Xianghui Yu, Liangren Zhang, Lihe Zhang, Lihe Zhang, Lihe Zhang
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.
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