Table 2.
Inhibitory Activity of ProTides against HIV-1 in human tonsillar tissues ex vivo.
| Cps | Nucl | ProTide | Aryl | Amino Acid |
Ester | Anti-HIV Activity EC50 (µM) |
|---|---|---|---|---|---|---|
| 28 Cf3375 | 1 | Mono | Naph | L-Ala | Bn | 11 |
| 42 Cf2985 | 2 | Mono | Ph | L-Ala | Bn | >20 |
| 66 Cf2933 | 5 | Mono | Ph | L-Ala | Bn | 0.9 |
| 74 Cf2911 | 1 | Cyclic | - | L-Ala | Et | 4.6 |
| 55 Cf3110 | 3 | Bis | Ph | L-Ala | Bn | >3 |
| 60 Cf3583 | 4 | Mono | Ph | L-Ala | Bn | 4 |
| 74 Cf3584 | 4 | Cyclic | - | L-Ala | Bn | 9 |
| 76–77 Cf3595 | MonoAcetyl 4 | - | - | - | - | >10 |
| 78–79 Cf3597 | MonoAcetyl 4 | Mono | Ph | L-Ala | Bn | 4 |
| 1 GCV | - | - | - | - | - | 5 |
| 2 PCV | - | - | - | - | - | 11 |
| 3 Cf2937 | - | - | - | - | - | >30 |
| 4 Cf2936 | - | - | - | - | - | >60 |
| 5 Cf2932 | - | - | - | - | - | >30 |