Table 2.
Evaluation of the antiviral activity against human immunodeficiency virus (HIV) and cytotoxicity against PBM, CEM, and VERO cells in vitro, expressed in μM, of synthesized AZT and FLT analogues
| Compound | Anti-HIV-1 activity in PBMCs (EC50) | Toxicity (IC50) | ||
|---|---|---|---|---|
| PBM | CEM | VERO | ||
| AZTa | 0.016 | >100 | 14.0 | 29.0 |
| 12 | 6.9 | 25.6 | 15.1 | 22.9 |
| 10a | 3.1 | 43.0 | 100 | 82.7 |
| 10b | 0.6 | 26.8 | 31.6 | 29.5 |
| 10c | 4.9 | 18.4 | 33.1 | 18.5 |
| 18 | 2.3 | 19.7 | 31.6 | 14.4 |
| 16a | 3.4 | 18.6 | 30.7 | 52.3 |
| 16b | 1.1 | 26.2 | 30.6 | 27.7 |
| 16c | 2.7 | 23.8 | 48.1 | 9.0 |
Reference compound.