doi: 10.1016/s0166-3542(01)00209-1.
Antiviral activity of UIC-PI, a novel inhibitor of the human immunodeficiency virus type 1 protease
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- PMID: 11888655
- DOI: 10.1016/s0166-3542(01)00209-1
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Antiviral activity of UIC-PI, a novel inhibitor of the human immunodeficiency virus type 1 protease
Antiviral Res.
2002 Apr.
Abstract
The human immunodeficiency virus type 1 (HIV-1) protease inhibitor UIC-PI (1) was developed via structure-based design and incorporated a novel bis-tetrahydrofuran (bis-THF) ligand in the (R)-(hydroxyethyl)sulfonamide based isostere. The EC(50) and EC(90) of the compound in acutely-infected H9 cells were <1 and approximately 1 nM, respectively. In chronically infected H9/HIV-1(IIIB) cells, the EC(50) and EC(90) were 20 and 50 nM, respectively. In parallel studies comparing UIC-PI and saquinavir in H9/HIV-1(IIIB) cells, viral p24 levels in culture supernatants were an order of magnitude lower with UIC-PI than with saquinavir.
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