Table 1.
Antiviral activity of compounds 1–33 in influenza virus-infected MDCKa cell cultures.
| Compound | Anti-influenza activity: EC50b (μM) |
Cytotoxicity (μM) |
||||||
|---|---|---|---|---|---|---|---|---|
| A/Virginia/ATCC3/2009 (H1N1) |
A/Ned/378/05 (H1N1) |
B/Ned/537/05 |
||||||
| CPE | MTS | CPE | MTS | CPE | MTS | MCCc | CC50d | |
| 1 | 28 | 17 | 33 | 29 | 2.2 | 1.1 | ≥4 | 52 |
| 2 | 40 | 28 | 43 | 14 | 4.0 | 1.2 | ≥4 | >100 |
| 3 | 53 | 34 | 48 | 34 | 11 | 1.2 | ≥4 | >100 |
| 4 | 59 | 49 | 63 | 37 | 8.2 | 2.0 | 14 | >100 |
| 5 | 59 | 36 | 41 | 24 | 8.4 | 1.5 | ≥4 | >100 |
| 6 | 39 | 19 | 21 | 7.3 | 2.9 | 1.0 | ≥4 | 53 |
| 7 | >83 | >83 | >100 | >100 | 35 | 7.8 | ≥100 | >100 |
| 8 | >83 | >83 | >100 | >100 | >100 | >100 | 100 | >100 |
| 9 | >83 | >83 | >100 | >100 | >100 | >100 | >100 | >100 |
| 10 | 34 | >83 | >100 | >100 | 56 | 19 | ≥100 | >100 |
| 11 | 1.0 | 0.67 | 1.1 | 0.85 | 0.10 | 0.040 | ≥0.2 | 1.4 |
| 12 | >100 | 21 | Nt | nt | 1.7 | 0.2 | ≥0.8 | >100 |
| 13 | >100 | >100 | Nt | nt | 0.016 | 0.015 | ≥0.03 | 29 |
| 14 | 1.0 | 1.0 | 1.1 | 0.60 | 0.015 | 0.007 | ≥0.2 | 6.1 |
| 15 | ≥83 | >83 | >100 | >100 | >100 | >100 | >100 | >100 |
| 16 | 1.4 | 0.72 | 0.55 | 0.35 | 0.080 | 0.030 | ≥0.2 | 6.7 |
| 17 | >100 | 36 | Nt | nt | 1.8 | 0.8 | ≥0.8 | >100 |
| 18 | >83 | >83 | >100 | >100 | 8.3 | 2.2 | ≥20 | >100 |
| 19 | 33 | 24 | 45 | 68 | 2.8 | 1.0 | ≥4 | >100 |
| 20 | >83 | >83 | >100 | >100 | 18 | 6.1 | ≥20 | >100 |
| 21 | >100 | 49 | Nt | nt | 4.5 | 0.4 | ≥0.8 | >100 |
| 22 | >100 | >100 | Nt | nt | 1.6 | 0.33 | ≥0.8 | >100 |
| 23 | 10 | 49 | >100 | >100 | >83 | 36 | >100 | >100 |
| 24 | >100 | >100 | Nt | nt | 10 | 3.0 | ≥20 | >100 |
| 25 | >100 | >100 | Nt | nt | 19 | 4.4 | ≥20 | >100 |
| 26 | >83 | >83 | >100 | >100 | 17 | 4.9 | ≥20 | >100 |
| 27 | >83 | >83 | >100 | >100 | 29 | >100 | >100 | >100 |
| 28 | >83 | >83 | >100 | >100 | >100 | >100 | 62 | >100 |
| 29 | >83 | >83 | >100 | >100 | >100 | >100 | >100 | >100 |
| 30 | >83 | >83 | >100 | >100 | >100 | >100 | 100 | >100 |
| 31 | >83 | >83 | >100 | >100 | >100 | >100 | >100 | >100 |
| 32 | >83 | >83 | 15 | 35 | 2.0 | 1.1 | ≥4 | 41 |
| 33 | >83 | >83 | >100 | >100 | >100 | >100 | >100 | >100 |
| Amantadine | 124 | 211 | 2.3 | 2.2 | >400 | >400 | >400 | >400 |
| Rimantadine | >400 | >400 | 0.32 | 0.050 | >400 | >400 | >400 | >400 |
| Ribavirin | 8.4 | 19 | 10 | 7.6 | 4.9 | 3.9 | ≥100 | >100 |
| Zanamivir | 2.3 | 6.8 | 0.80 | 0.20 | 0.060 | 0.055 | >100 | >100 |
a
MDCK: Madin-Darby canine kidney cells.
b
EC50: 50% effective concentration producing 50% inhibition of virus-induced cytopathic effect (CPE), as determined by microscopy or by measuring the cell viability with the colorimetric formazan-based MTS assay.
c
MCC: minimum compound concentration producing a microscopically detectable alteration in normal cell morphology.
d
CC50: 50% cytotoxic concentration, as determined by measuring the cell viability with the colorimetric formazan-based MTS assay. Values shown are the mean of 3–6 determinations. nt = not tested.