Table 3.
Antiviral properties against HSV, vaccinia virus and adenovirus.
| Compounds | EC50a (μM) |
Cytotoxicity (μM) |
|||||
|---|---|---|---|---|---|---|---|
| HSV-1 |
HSV-2 (G) | Vaccinia virus | Human Coronavirus (229E) | MCCb | CC50c | ||
| (KOS) | (TK-KOS ACVr) | ||||||
| 19 | 9.6 ± 4.7 | 3.2 ± 3.2 | 5.3 ± 4.2 | >100 | 24.6 ± 18.5 | >100 | >83 ± 24 |
| 20 | 11.5 ± 4.7 | 4.1 ± 5.1 | 2.9 ± 3.4 | >100 | 60 ± 35 | >100 | 55 ± 3 |
| 21 | 59.0 ± 19.8 | 23.5 ± 16.3 | 31.0 ± 4.1 | >100 | >100 | >100 | >100 |
| 22 | >100 | >100 | >100 | >100 | >100 | >100 | >100 |
| 23 | >100 | 79.0 ± 29.7 | >100 | >100 | 45 ± 0 | >100 | ND |
| 24 | 43 ± 21 | 24 ± 6 | 40 ± 8 | >100 | 8.9 ± 0 | >100 | ND |
| 1 (R1 = Me) | 3.1 ± 1.4 | 9.2 ± 7.2 | 6.5 ± 3.4 | 30.7 ± 14.5 | NDd | ≥100 | 36.4 ± 2.3 |
| 2 (R1 = Me) | 4.2 ± 0.7 | 2.8 ± 1.2 | 6.1 ± 2.9 | >200 | ND | >200 | 36 |
| 3 (R1 = Me) ( | >152 | >152 | >152 | ND | ND | >152 | 14.7 |
| 4 (R1 = Me) | >37 | >37 | >37 | >37 | ND | 184 | 76 |
| Acyclovir | 1.2 ± 1.1 | 94 ± 25 | 0.7 ± 0.7 | >250 | – | >440 | >440 |
| Brivudine | 0.081 ± 0.034 | 420 ± 280 | 169 ± 116 | 10.8 9.4 | – | >300 | >300 |
| Cidofovir | 6.5 ± 3.7 | 4.6 ± 2.7 | 4.1 ± 2.7 | 21.3 ± 3.8 | – | >300 | >300 |
| UDA | – | – | – | – | 5.4 ± 5.0 μg/mL | >100 | – |
a
Effective concentration required to viral cytopathic effect by 50%.
b
Minimum cytotoxic concentration that causes a microscopically detectable alteration of cell morphology.
c
Cytostatic concentration required to reduce cell growth by 50%.
d
Not done.