Table 1.
A comparison of cell-culture versus in vitro HIV-1 RT inhibition (μM) for double-drugs 15a-d and 17.
| Compound | Cell-Culture EC501 (μM) | Cell-Culture CC502 (μM) | RT Assay3 (μM) |
|---|---|---|---|
| HI-236 | 0.042 | >1 | 0.038 ± 0.007 |
| d4T | 2.3 | >100 | 9.64 |
| 15a | 0.25 | 17 | 0.061±0.015 |
| 15b | 1.3 | 38 | 0.575 ± 0.14 |
| 15c | 1.9 | 43 | 0.850 ± 0.14 |
| 15d | 3.1 | 18 | 1.4 ± 0.5 |
| 17 | 2.9 | 11 | 2.3 ± 0.8 |
 |
12041 | N/A |
1
effective concentration that inhibits viral-mediated T-cell death by 50%, determined by averaging samples of each concentration in triplicate.
2
concentration that kills 50% of the T-cells, also determined by averaging triplicate samples.
3
concentration of inhibitor that inhibits by 50% the steady-state thymidine incorporation into a D23 / D36 primer-template as catalysed by RT.
4
Based on pre-steady-state kinetic analysis.