TABLE 2.
Anti-HIV activity of Cf-1093 and Cf-1001, the aryloxyphosphoramidate prodrug derivatives of ddA- and d4A-MP, respectivelya
| Compound | EC90 (μM) for M/M | EC50 (μM) for:
|
CC50b (μM) for:
|
SIc of M/M | ||
|---|---|---|---|---|---|---|
| M/M | CEM | M/M | CEM | |||
| ddA | NAd | 1 ± 0.5 | 3.7 ± 2.1 | 60 | >250 | 60 |
| Cf-1093 | 0.02 ± 0.003 | 0.004 ± 0.001 | 0.016 ± 0.0 | 10 | 2.6 ± 0.64 | 2500 |
| d4A | NA | 5 ± 1 | 29 ± 19 | 50 | 95 ± 7.1 | 10 |
| Cf-1001 | 0.03 ± 0.005 | 0.008 ± 0.003 | 0.006 ± 0.0007 | >5e | 3.75 ± 0.92 | 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.
d
NA, not achieved.
e
A higher concentration could not be tested due to DMSO toxicity. The stock solution of Cf-1001 was made in DMSO at a lower Cf-1001 concentration than those for the other compounds.