Indolizine Derivatives as HIV-1 VIFElonginC Interaction Inhibitors

Compound 1 (VEC-5) was identified as a potent small-molecular HIV-1 viron infectivity factor inhibitor that targets the viron infectivity factorElonginC interaction. A structureactivity 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 11.0m. These results provide new information to develop highly potent small-molecule HIV-1 viron infectivity factor inhibitors.Biochemistry & Molecular BiologyChemistry, MedicinalSCI(E)PubMed4ARTICLE6730-7418