TABLE 1.
Inhibition of wt and drug-resistant HIV-1 variants by UC781, AZT, and a 1:1 molar ratio combination of UC781 and AZT
| HIV-IIIB variant | EC50 (nM)a
|
||
|---|---|---|---|
| AZT | UC781 | AZT plus UC781 | |
| wt | 5.3 ± 1.25 | 10.4 ± 5 | 2.8 ± 1.4 |
| UC781 resistant | 6.6 ± 3.3 | 16,600 ± 2,300b | 11.0 ± 4.6 |
| AZT resistant | >2,500c | 13.1 ± 4 | 3.8 ± 0.8 |
a
EC50 was assessed by measuring p24 antigen levels in culture supernatants and by assessment of syncytium formation. The values are the means ± standard deviations from at least three separate experiments, each of which was carried out in triplicate.
b
UC781 showed no cytotoxic activity at concentrations up to 100 μM (the highest concentration tested in these experiments).
c
Concentrations of AZT higher than 2.5 μM were cytotoxic.