TABLE 2.
Efficacies and cytotoxicities of PMEA 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 | |||
| PMEA | GS 0393 | >366 ± 0 | >366 ± 0 | — | >366 ± 0 | — |
| Bis[(pivaloyl)oxymethyl]PMEA | GS 0840 | 117 ± 27 | 5.1 ± 0.7 | 23 | 13 ± 8.8 | 9.0 |
| Bis (butyl-l-alaninyl)PMEA | GS 8357 | 100 ± 27 | 4.4 ± 0.2 | 23 | 10 ± 8.2 | 10 |
| PMEDAP | GS 0573 | >339 ± 12 | 204 ± 15 | 1.7 | >347 ± 0 | — |
| PME-N6-(cyclopropyl)DAP | GS 8369 | >263 ± 59 | 23 ± 6.9 | >11 | 28 ± 13 | >9.4 |
| Bis(butyl-l-alaninyl)PME-N6-(cyclopropyl)DAP | GS 8361 | 49 ± 33 | 0.08 ± 0.01 | 613 | 0.26 ± 0.2 | 189 |
| (Isopropyl-l-alaninyl)phenyl-PME-N6-(cyclopropyl)DAP | GS 17432 | >209 ± 69 | 1.1 ± 0.3 | >190 | 2.6 ± 1.9 | >80 |
| PME-N6-(trifluoroethyl)DAP | GS 8367 | >270 ± 0 | 42 ± 11 | >6.4 | >270 ± 0 | — |
| PME-N6-(dimethyl)DAP | GS 8368 | >316 ± 0 | 35 ± 1.6 | >9.0 | 53 ± 8.3 | >6.0 |
| PME-N6-(2-propenyl)DAP | GS 8370 | >305 ± 0 | 25 ± 0.9 | >12 | 115 ± 78 | >2.7 |
a
GS, Gilead Sciences.
b
Values are the means of two or more assays ± standard deviation.
c
SI = CC50/EC50.