TABLE 1.
Effects of nucleoside analogs on BV TK activity (IC50)a
| Nucleoside analog | Acronym | IC50 (μM) (mean ± SD)b |
|---|---|---|
| Thymidine analogs | ||
| 5-Trifluoromethyl-2′-deoxyuridine | TFT | 2.0 ± 0.1 |
| l-Thymidine | l-TdR | 4.1 ± 0.02 |
| E-5-(Bromovinyl)deoxyuridine | BVdU | 32.3 ± 3.5 |
| l-5-(Bromovinyl)deoxyuridine | l-BVdU | 15.0 ± 2.0 |
| 5-Iododeoxyuridine | IUdR | 1.5 ± 0.2 |
| l-5-Iodo-2′-deoxyuridine | l-IUdR | 2.0 ± 0.2 |
| 5-Ethyl-2′-deoxyuridine | Et-dU | 0.15 ± 0.01 |
| α-5-Ethyl-2′-deoxyuridine | α-Et-dU | 52 ± 5.0 |
| 5-Propyl-2′-deoxyuridine | Pr-dU | 4.2 ± 0.2 |
| Acyclonucleosides | ||
| Acyclovir | ACV | 1,000 ± 210 |
| Ganciclovir | GCV | 800 ± 112 |
| Cidofovir | CFV | 900 ± 155 |
| Penciclovir | PCV | 84.4 ± 5.5 |
| 2-Amino-9-(4-hydroxybutyl)-6-oxopurine | HBG | 177 ± 20 |
| HSV TK inhibitors | ||
| N2-(3-Trifluoromethylphenyl)guanine | CF3PG | 3.5 ± 0.15 |
| 2-Phenylamino-9-(4-hydroxy-butyl)-6-oxopurine | HBPG | 11.5 ± 1.0 |
| 2-Phenylamino-9-(N,N-dimethylaminobutyl)-6-oxopurine | DMBPG | 1.2 ± 0.15 |
a
Enzyme assays contained 1 μM [3H]TdR and were run in duplicate with at least five concentrations of inhibitor.
b
The values are the means for two independent experiments in which each concentration was tested in duplicate.