Table 4.
In vitro activity of aaptamine and derivatives (1, 2, 5-30) against HIV-1 in Human PBM cells with host cytotoxicity (PBM). For some compounds, endpoints were not pursued if cytotoxicity was high
| Cytotoxicity (IC50, μM)a,b |
||||
|---|---|---|---|---|
| Compound | HIV-1 EC50 (μM)a,b | PBM | CEM | Vero |
| 1 | 8.9 | <1.0 | 3.3 | 23.1 |
| 2 | 7.7 | 1.1 | 1.4 | 2.1 |
| 5 | NA | 21.2 | NC | NC |
| 6 | 39.0 | 31.6 | 60.3 | 58.4 |
| 7 | 35.6 | 11.7 | 69.0 | 46.8 |
| 8 | NA | 95.7 | NC | NC |
| 9 | 4.0 | 4.3 | 7.6 | 74.3 |
| 10 | 24.2 | 1.4 | 23.8 | NC |
| 11 | NA | 3.2 | 5.3 | 11.8 |
| 12 | 36.7 | 13.7 | 5.7 | NC |
| 13 | 31.6 | 2.6 | 16.3 | 17.6 |
| 14 | 31.6 | 2.3 | 10.9 | 17.2 |
| 15 | NA | 3.2 | 5.3 | 11.8 |
| 16 | 7.4 | 2.2 | 3.8 | 3.7 |
| 17 | 22.4 | 1.1 | 3.5 | 3.9 |
| 18 | 48.4 | 1.4 | 1.2 | 2.1 |
| 19 | NA | 3.2 | <1.0 | 7.1 |
| 20 | 3.02 | <1.0 | <1.0 | <1.0 |
| 21 | NA | <1.0 | <1.0 | <1.0 |
| 22 | <1.0 | 1.5 | 1.8 | 2.2 |
| 23 | 4.2 | 1.8 | 7.3 | 3.5 |
| 24 | 6.2 | 1.0 | 6.0 | 9.0 |
| 25 | 3.6 | 2.3 | 1.3 | 13.4 |
| 26 | 8.1 | 10.4 | 2.0 | 27.3 |
| 27 | 0.54 | <1.0 | <1.0 | 1.2 |
| 28 | 0.52 | 1.1 | <1.0 | 1.3 |
| 29 | 67.1 | NC | NC | NC |
| 30 | 2.8 | 3.3 | 3.8 | 9.1 |
a
HIV-1 EC50 Control (AZT) = 0.0048 μM (NC).
b
NA/NC = Not Active/Cytotoxic at >100 μM.