Table 2.
Effect of analogs against HIV-1 (strain LA1) in human peripheral blood mononuclear (PBM) cells
| Anti-HIV-1 activity in PBM cellsa | Cytotoxicity (IC50, μM)b | |||||
|---|---|---|---|---|---|---|
| Analog | Base | EC50, μM | EC90, μM | PBM cells | CEM cells | VERO cells |
| AZT | β-T0 | 0.0015 | 0.006 | > 100 | 14.3 | 50.6 |
| 20a+21a | α/β-U | 60.7 | > 100 | > 100 | > 100 | > 100 |
| 20b+21b | α/β-T | 82.02 | > 100 | > 100 | > 100 | > 100 |
| 20d+21d | α/β-BVU | > 100 | > 100 | > 100 | > 100 | > 100 |
| 20e+21e | α/β-N-Ac-C | > 100 | > 100 | > 100 | > 100 | > 100 |
| 20g+21g | α/β-2,6-di-Cl-purine | 24.6 | 62.4 | 43.1 | 5.9 | 18.9 |
| 22a | β-U | 90.5 | > 100 | > 100 | 67.0 | > 100 |
| 22b | β-T | > 100 | > 100 | > 100 | > 100 | > 100 |
| 22c | β-5-F-U | > 100 | > 100 | > 100 | > 100 | > 100 |
| 22d | β-BVU | 77.8 | > 100 | > 100 | > 100 | > 100 |
| 22f | β-6-Cl-purine | 70.3 | > 100 | > 100 | 95.6 | > 100 |
| 22i | β-A | > 100 | > 100 | > 100 | > 100 | > 100 |
| 22j | β-2-Cl-A | 16.5 | 39.1 | 27.2 | > 100 | 34.7 |
| 22l | β-2-Cl-6-OMe-purine | 20.2 | 95.6 | > 100 | > 100 | 76.2 |
| 22m | β-2,6-di-NH2-purine | > 100 | > 100 | > 100 | > 100 | > 100 |
| 22o | β-I | 12.3 | 44.3 | 41.4 | 20.1 | 50.3 |
| 23b | α-T | > 100 | > 100 | > 100 | > 100 | > 100 |
| 23d | α-BVU | 19.0 | 74.2 | 31.9 | 34.2 | 19.6 |
| 23f | α-6-Cl-purine | 28.5 | 46.9 | 54.2 | 21.9 | 98.3 |
| 23i | α-A | 90.6 | > 100 | > 100 | ≥ 100 | > 100 |
| 23j | α-2-Cl-A | 36.2 | 67.1 | 30.6 | > 100 | 61.9 |
| 23m | α-2,6-di-NH2-purine | > 100 | > 100 | ≥ 100 | > 100 | > 100 |
| 24b | α/β-T | > 100 | > 100 | > 100 | > 100 | > 100 |
| 24h | α/β-C | > 100 | > 100 | > 100 | > 100 | > 100 |
| 24i | α/β-A | > 100 | > 100 | > 100 | > 100 | > 100 |
| 24j | α/β-2-Cl-A | 76.2 | > 100 | > 100 | > 100 | > 100 |