TABLE 1.
Anti-HIV activity of So221 and So324, the aryloxyphosphoramidate prodrug derivatives of AZT- and d4T-MP, respectivelya
| Compound | EC90 (μM) for M/M | EC50 (μM) for:
|
CC50b (μM) for:
|
SIc of:
|
|||
|---|---|---|---|---|---|---|---|
| M/M | CEM | M/M | CEM | M/M | CEM | ||
| d4T | 0.78 ± 0.02 | 0.20 ± 0.05 | 0.35 ± 0.07 | >100 | 143 ± 1.4 | >500 | 497 |
| So324 | 0.03 ± 0.001 | 0.008 ± 0.001 | 0.07 ± 0.007 | >100 | ≥100 | >12,500 | ≥769 |
| AZT | 0.02 ± 0.003 | 0.005 ± 0.001 | 0.002 ± 0.002 | >100 | >100 | >20,000 | >33,300 |
| So221 | 0.1 ± 0.02 | 0.012 ± 0.005 | 0.06 ± 0.02 | >100 | >100 | >8,300 | >12,500 |
a
Results are presented as means ± standard deviations of tree values obtained in four different experiments.
b
CC50, 50% cytotoxic concentration.
c
SI = CC50/EC50.