TABLE 1.
Efficacies and cytotoxicities of HPMPC and related ANPs against VV and CV in HFF
| Compound | GS no.a | CC50 (μM)b | VV
|
CV
|
||
|---|---|---|---|---|---|---|
| EC50 (μM)b | SIc | EC50 (μM) | SI | |||
| HPMPC (CDV) | GS 0504 | 278 ± 9.2 | 33 ± 9.1 | 8.4 | 43 ± 2.5 | 6.5 |
| cHPMPC | GS 0930 | >302 ± 0 | 38 ± 11 | >7.9 | 48 ± 8.0 | >6.3 |
| (S)-HPMPA | GS 0577 | 269 ± 21 | 3.5 ± 2.8 | 77 | 5.0 ± 4.7 | 54 |
| 2-(Butyloxycarbonyl)phenylcHPMPC | GS 3857 | >213 ± 22 | 32 ± 13 | >6.7 | 34 ± 4.2 | >6.3 |
| (Butyl-l-alaninyl)cHPMPC | GS 8262 | >153 ± 57 | 4.6 ± 0.8 | >33 | 8.4 ± 5.3 | >18 |
| (Phenethyl-l-alaninyl)cHPMPC (mixed diastereomers) | GS 7356 | 207 ± 18 | 7.1 ± 0.3 | 29 | 6.8 ± 1.8 | 30 |
| (Ethyl-l-alaninyl)cHPMPC (isomer I) | GS 7357 | >276 ± 23 | 15 ± 13 | >18 | 27 ± 6.5 | >10 |
| (Ethyl-l-alaninyl)cHPMPC (isomer II) | GS 7358 | >278 ± 0 | 15 ± 11 | >19 | 26 ± 3.5 | >11 |
a
GS, Gilead Sciences.
b
Values are the means of two or more assays ± standard deviation.
c
SI = CC50/EC50.