Table 6.
Inhibitory activity of acyclic α-CNPs in herpetic DNA polymerase assays using different dNTP substrates
| Nucleobase | Compound | IC50a (μM)
|
||||
|---|---|---|---|---|---|---|
| HCMV DNA polymeraseb
|
VZV DNA polymerasec
|
|||||
| [3H]dATP | [3H]dCTP | [3H]dGTP | [3H]dTTP | [3H]dTTP | ||
| Thymine | 6g | 3.1 ± 1.1 | 3.0 ± 0.4 | 2.5 ± 0.3 | 2.1 ± 0.6 | 2.2 ± 0 |
| Adenine | 6k | 3.0 ± 2.0 | 2.9 ± 0.9 | 3.2 ± 0.4 | 5.5 ± 2.1 | 3.3 ± 0 |
| Guanine | 6l | 10 ± 12 | 11 ± 1 | 14 ± 11 | 3.6 ± 0.6 | 2.9 ± 0 |
| Cytosine | 6m | 33 ± 5 | 20 ± 14 | 30 ± 4 | 16 ± 8 | 2.9 ± 0 |
a
50% Inhibitory concentration.
b
Template/primer: activated calf thymus DNA; [3H]dNTP substrate + three non-radiolabeled dNTPs.
c
Template/primer: poly dA.oligo dT; [3H]dTTP substrate.