TABLE 1.
Antiviral activity, cellular cytotoxicity, and selectivity index of a novel series of compounds in Vero cellsa
| Compound | EC50 (μΜ)b |
CC50 (μΜ)c | SId |
||
|---|---|---|---|---|---|
| DENV2 | ZIKV | DENV2 | ZIKV | ||
| 15a | 19.4 ± 7.5 | 40 ± 3.8 | 41.8 ± 9.8 | 2.1 | 1 |
| 15b | 18.6 ± 3.5 | 12.1 ± 1.7 | >100 | 5.4 | 8.3 |
| 20 | 5.9 ± 3.9 | >100 | >100 | >17 | >1 |
| 21 | 37.1 ± 6.0 | 4.0 ± 2.0 | >100 | >2.7 | >25 |
| 22 | 2.8 ± 2.8 | >100 | >100 | >35.7 | >1 |
| 24 | 0.4 ± 0.2 | 0.2 ± 0.1 | 80 ± 35 | 200 | 400 |
| cis−10 | 1.0 ± 0.2 | 0.8 ± 0.1 | >100 | >100 | >125 |
| trans−10 | 2.7 ± 0.9 | 12 ± 3.8 | >100 | >37 | >8.3 |
| cis−11 | 10.9 ± 1.7 | 7.2 ± 1.4 | 27.7 ± 9.4 | 2.5 | 3.8 |
| cis−12 | 0.3 ± 0.1 | 36.2 ± 6.5 | >100 | >333 | >2.7 |
| cis−13 | 1.1 ± 0.2 | 3.3 ± 0.5 | 5.8 ± 0.1 | 5.3 | 1.8 |
| trans−13 | 4.0 ± 2.8 | 6.5 ± 0.2 | 9.2 | 2.3 | 1.4 |
| trans−14 | 2.8 ± 1.9 | >100 | >100 | >35.7 | >1 |
a
The laboratory-adapted viral strains DENV2 NGC and ZIKV MR766 were used.
b
EC50, effective concentration of the compound able to inhibit viral replication by 50%, as assessed by qRT-PCR of supernatants at 72 h p.i.
c
CC50, concentration of the compound required to reduce cell viability by 50%, as assessed by MTS analysis of cell lysates at 72 h p.i.
d
SI, selectivity index (CC50/EC50).