Table 1.
Effects of various nucleosides and their conjugates 10a-h against HIV-1 and their cytotoxicity assays.
| Analog | Nucleoside/Conjugate (source) | Anti-HIV-1 activity in PBM cellsa |
Cytotoxicity (IC50 [μM])b |
|||
|---|---|---|---|---|---|---|
| EC50 [μM] | EC90 [μM] | PBM cells | CEM cells | VERO cells | ||
| AZT | (commercial) | 0.0054 | 0.050 | > 100 | 14.3 | 56.0 |
| d4U | (synthesized) | > 100 | > 100 | > 100 | 55.9 | > 100 |
| 10a | Glc-d4U | > 100 | > 100 | > 100 | > 100 | > 100 |
| d4T | (commercial) | 0.073 | 0.37 | |||
| d4T | (synthesized) | 0.069 | 0.37 | > 100 | > 100 | > 100 |
| 10b | Glc-d4T | 0.34 | 2.0 | > 100 | 76.8 | > 100 |
| IdUrd | (commercial) | 65.7 | > 100 | |||
| IdUrd | (synthesized) | 86.5 | > 100 | > 100 | 2.7 | > 100 |
| 10c | Glc-5′-IdUrd | 32.4 | > 100 | > 100 | 2.3 | > 100 |
| 10d | Glc-3′-IdUrd | > 100 | > 100 | > 100 | 76.0 | > 100 |
| ddI | (commercial) | 0.32 | 2.8 | |||
| ddI | (synthesized) | 0.06 | 0.76 | > 100 | > 100 | > 100 |
| 10e | Glc-ddI | 15.5 | > 100 | > 100 | 22.7 | > 100 |
| ddA | (synthesized) | 0.59 | 3.8 | > 100 | > 100 | > 100 |
| 10f | Glc-ddA | 1.1 | 9.9 | 87.6 | 13.2 | 73.2 |
| Virazole | (commercial) | 77.5 | > 100 | |||
| Virazole | (synthesized) | 85.9 | > 100 | > 100 | 53.0 | > 100 |
| 10g | Glc-Virazole | 12.8 | 39.1 | > 100 | 17.6 | > 100 |
| Ara-A | (commercial) | > 100 | > 100 | |||
| Ara-A | (synthesized) | > 100 | > 100 | 26.0 | 26.2 | > 100 |
| 10h | Glc-Ara-A | 19.5 | > 100 | > 100 | 18.9 | > 100 |
| Ara-C | (synthesized) | 4.9 | 11.9 | 57.0 | < 0.1 | ND |
| 10i | Glc-Ara-C | 5.8 | 14.0 | 17.5 | < 1.0 | < 1.0 |