Table 5.
Inhibitory activity of acyclic α-CNP derivatives carrying different pyrimidine or purine bases against viral and human DNA polymerases.
| Compound | IC50a (μM)
|
|||||
|---|---|---|---|---|---|---|
| HIV-1 RT | HCMV DNA Pol | HSV-1 DNA Pol | VZV DNA Pol | Human DNA Pol α | Human DNA Pol β | |
| 6g | 235±16 | 2.1±0.6 | 3.7±1.7 | 2.2±0.1 | 14±7 | >500 |
| 6h | 145±106 | 29±3 | 45±27 | 27±12 | 301±51 | 450±105 |
|
| ||||||
| 6i | >500 | 30±16 | 24±1 | 27±2 | 325±4 | >500 |
| 6j | 263±69 | 9.4±4.1 | 6.7±4.6 | 4.1±0.9 | 72±52 | 306±3 |
| 6k | 404±30 | 5.5±2.1 | 2.7±2.0 | 3.3±0.4 | ≥500 | 454±28 |
| 6l | ≥500 | 3.6±0.6 | 2.1±2.3 | 2.9±0.0 | 365±91 | >500 |
| 6m | 270±33 | 16±8 | 12±6 | 2.9±0.9 | 414±22 | >500 |
|
| ||||||
| Thymine α-CNP | 0.40±0.05 | 38±11 | 26±20 | 38±16 | 229±27 | >500 |
a
IC50 or 50% inhibitory concentration.