Table 3.
Cytotoxicity and antiviral activity against cytomegalovirus in HEL cell cultures
| Compound | R | Antiviral activity EC50a (μM) |
Cytotoxicity (μM) | |
|---|---|---|---|---|
| AD-169 strain | Davis strain | Cell morphology MCCb | ||
| cis-9a |  |
|||
| (exp. 1) | 45 | 45 | >100 | |
| (exp. 2) | 45 | 45 | >100 | |
| trans-9a | ||||
| (exp. 1) | >20 | 55 | >100 | |
| (exp. 2) | 49 | 45 | >100 | |
| cis-9b |  |
|||
| (exp. 1) | >20 | >20 | 100 | |
| (exp. 2) | >20 | >20 | 100 | |
| trans-9b | ||||
| (exp. 1) | >20 | >20 | 100 | |
| (exp. 2) | >20 | >20 | 100 | |
| cis-9c |  |
|||
| (exp. 1) | 45 | 45 | >100 | |
| (exp. 2) | 45 | 45 | >100 | |
| trans-9c | ||||
| (exp. 1) | >100 | >100 | >100 | |
| (exp. 2) | >100 | >100 | >100 | |
| cis-9d |  |
|||
| (exp. 1) | 45 | 41 | >100 | |
| (exp. 2) | 37 | 37 | >100 | |
| trans-9d | ||||
| (exp. 1) | 8.9 | 8.9 | 100 | |
| (exp. 2) | 8.9 | 8.9 | 100 | |
| cis-9e |  |
|||
| (exp. 1) | 100 | 100 | >100 | |
| (exp. 2) | 100 | >100 | >100 | |
| trans-9e | ||||
| (exp. 1) | 55 | 49 | >100 | |
| (exp. 2) | 55 | 63 | >100 | |
| cis-9f |  |
|||
| (exp. 1) | 45 | 45 | >100 | |
| (exp. 2) | 45 | 45 | >100 | |
| trans-9f | ||||
| (exp. 1) | 8.9 | 10.9 | 100 | |
| (exp. 2) | 10.9 | 20 | 100 | |
| Cidofovir | ||||
| (exp. 1) | 0.92 | 1.02 | >350 | |
| (exp. 2) | 0.92 | 1.14 | >350 | |
| Ganciclovir | ||||
| (exp. 1) | 7.1 | 7.1 | >350 | |
| (exp. 2) | 6.3 | 7.9 | >350 | |
a
Effective concentration required to reduce virus plaque formation by 50%. Virus input was 100 plaque forming units (PFU).
b
Minimum cytotoxic concentration that causes a microscopically detectable alternation of cell morphology.