TABLE 2.
Antiviral activity of QYL-685 and QYL-609 against wild-type and drug-resistant infectious HIV-1
| Compound | IC50 (μM)a for:
|
|||
|---|---|---|---|---|
| HIV-1wtb | HIV-1215 | HIV-174 | HIV-162/75/77/116/151 | |
| AZT | 0.017 ± 0.004 | 0.14 ± 0.031 (10×)c | 0.023 ± 0.005 (1×) | 11 ± 5.2 (630×) |
| ddId | 3.7 ± 1.8 | 4.2 ± 1.1 (1×) | 25.4 ± 8.9 (7×) | 47 ± 8.3 (13×) |
| QYL-685 | 0.36 ± 0.054 | 0.30 ± 0.051 (1×) | 0.39 ± 0.25 (1×) | 0.39 ± 0.06 (1×) |
| QYL-609 | 0.029 ± 0.011 | 0.03 ± 0.01 (0.8×) | 0.013 ± 0.01 (0.5×) | 0.037 ± 0.02 (1×) |
a
MT-2 cells were exposed to 100 50% tissue culture infective doses of each infectious clone, the amounts of p24 Gag protein produced were determined by radioimmunoassay, and IC50s were computed (13, 17, 20, 21). Data shown represent the mean values (with standard deviations) derived from three independent experiments conducted in triplicate. All HIV-1 strains used were infectious clones as previously reported (22, 25).
b
HIV-1wt, wild-type HIV-1.
c
Numbers in parentheses indicate fold changes compared to the IC50 against HIV-1wt.
d
ddI, dideoxyinosine.