Table 7.
Inhibitory activity of acyclic α-CNPs in HIV-1 RT assays using different homopolymeric template/primer and dNTP testing conditions.
| Nucleobase | Compound | IC50a(μM)
|
|||
|---|---|---|---|---|---|
| Poly rA.dT ([3H]dTTP) | Poly rU.dA ([3H]dATP | Poly rI.dC ([3H]dCTP) | Poly rC.dG ([3H]dGTP) | ||
| Thymine | 6g | 235 ± 16 | ≥500 | >500 | >500 |
| Adenine | 6k | 404 ± 30 | 40 ± 8 | >500 | >500 |
| Guanine | 6l | ≥500 | 369 ± 48 | >500 | >500 |
| Cytosine | 6m | 270 ± 33 | >500 | 273 ± 54 | >500 |
|
| |||||
| ddTTP | - | 0.05 ± 0.01 | >20 | >20 | >20 |
| ddATP | - | >20 | 0.46 ± 0.12 | >20 | >20 |
| ddCTP | - | >20 | >20 | 3.1 ±2.2 | >20 |
| ddGTP | - | >20 | >20 | >20 | 0.26 ±0.17 |
| PFA | - | 0.34 ± 0.01 | 0.75 ± 0.13 | 6.8 ± 2.0 | 17 ± 2 |
a
50% Inhibitory concentration, obtained in the presence of homopolymeric template/primers and their corresponding [3H]dNTPs.