TABLE 1.
Activities of methylenecyclopropane analogues against HCMV and MCMV in HFF or MEF
| Drug | EC50 (μM) for HCMV
|
EC50 (μM) for MCMV
|
|||
|---|---|---|---|---|---|
| Determined by CPE inhibition assay | Determined by PR assay | SIa | Determined by PR assay | SI | |
| GCV | 0.39 | 2.3 | >170 | 2.0 | >19.6 |
| QYL-284A | 1.0 | 1.3 | >353 | 2.1 | >219 |
| QYL-438 | 0.04 | 1.2 | >358 | 0.3 | >1,430 |
| QYL-468 | 3.4 | 9.8 | >52.9 | 52.3 | >9.9 |
| QYL-546 | 11.2 | 15.9 | >27.1 | 0.6 | >488 |
| QYL-587A | 1.9 | 4.2 | >110 | 55 | >9.4 |
| QYL-678c | 7.6 | 25.0 | >8.2 | 3.3 | >62.4 |
| QYL-685d | 11.2 | 7.8 | 15.5 | 3.2 | 65.9 |
| QYL-769 | 2.0 | 2.4 | 136.3 | 0.37 | 595 |
| QYL-418 | 5.4 | 6.9 | 26.8 | 0.27 | 963 |
| QYL-788 | NTb | 1.9 | 94.7 | 0.55 | 538 |
| QYL-972e | 0.22 | 4.5 | 7.6 | 0.24 | 525 |
| QYL-941 | 1.5 | 5.3 | 76.2 | 0.4 | 650 |
| QYL-975f | 0.9 | 6.2 | 20.3 | 0.93 | 109 |
a
SI, selectivity index (CC50/EC50). EC50 values are from PR assays. CC50 values are obtained from Table 7.
b
NT, not tested.
c
Prodrug of QYL-438.
d
Prodrug of QYL-546.
e
Prodrug of QYL-941.
f
Prodrug of QYL-769.