Abstract
Bifunctional inhibitors were designed and synthesized based on 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT)a1 non-nucleoside reverse transcriptase (RT) inhibitors and diketoacid (DKA) integrase (IN) inhibitors. Biochemical studies revealed activity against RT and IN at low nanomolar and low micromolar concentrations, respectively. Exceptionally low IC50 values from a cell-based assay were achieved along with remarkably high therapeutic indices. Compound 7 was identified as the best compound of the series (IC50: 24 nM against RT, 4.4 μM against IN, and 10 nM against HIV-1).
| Original language | English (US) |
|---|---|
| Pages (from-to) | 3416-3419 |
| Number of pages | 4 |
| Journal | Journal of medicinal chemistry |
| Volume | 50 |
| Issue number | 15 |
| DOIs | |
| State | Published - Jul 26 2007 |
UN SDGs
This output contributes to the following UN Sustainable Development Goals (SDGs)
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SDG 3 Good Health and Well-being
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