Table 5.
Efficacy and cytotoxicity of acyclic nucleoside phosphonates against vaccinia virus and cowpox virus in HFF cells
| Compound | GS numbera | Vaccinia virus EC50 (μM) | Cowpox virus EC50 (μM) | Cytotoxicity CC50 (μM) |
| HPMPC (CDV) | GS 0504 | 33 ± 9.1 | 43 ± 2.5 | 278 ± 9.2 |
| Cyclic HPMPC (cHPMPC) | GS 0930 | 38 ± 11 | 48 ± 8.0 | >302 ± 0 |
| Butyl salicyl cyclic HPMPC | GS 3857 | 32 ± 13 | 34 ± 4.2 | >213 ± 22 |
| Phenethyl alaninyl cyclic HPMPC—mixture | GS 7356 | 7.1 ± 0.3 | 6.8 ± 1.8 | 207 ± 18 |
| Ethyl alaninyl cyclic HPMPC—isomer I | GS 7357 | 15 ± 13 | 27 ± 6.5 | >276 ± 23 |
| Ethyl alaninyl cyclic HPMPC—isomer II | GS 7358 | 15 ± 11 | 26 ± 3.5 | >278 ± 0 |
| HPMPA | GS 0577 | 3.5 ± 2.8 | 5.0 ± 4.7 | 269 ± 21 |
| PMEA | GS 0393 | >366 ± 0 | >366 ± 0 | >366 ± 0 |
| Bis(pivaloyloxymethyl)PMEA | GS 0840 | 5.1 ± 0.7 | 13 ± 8.8 | 117 ± 27 |
| Bis(butylalaninyl)PMEA | GS 8357 | 4.4 ± 0.2 | 10 ± 8.2 | 100 ± 27 |
| PMEDAP | GS 0573 | 204 ± 15 | >347 ± 0 | >339 ± 12 |
| PME(N6-cyclopropyl)DAP | GS 8369 | 23 ± 6.9 | 28 ± 13 | >263 ± 59 |
| Bis(butylalaninyl) PME(N6-cyclopropyl)DAP | GS 8361 | 0.08 ± 0.01 | 0.26 ± 0.2 | 49 ± 33 |
| PMPA | GS 1278 | >300 | >300 | >300 |
| Bis(isopropoxycarbonyloxymethyl)PMPA | GS 4331 | >157 | >157 | >157 |
| Isopropyl alaninylphenyl PMPA | GS 7340 | 23.5 | 98.9 | >143 |
| PMEG | GS 8358 | 4.0 ± 0.7 | 11.4 ± 1.3 | 88 |
a
Gilead sciences.