Table 4.
Cytotoxicity and antiviral activity against varicella-zoster virus (VZV) in HEL cell cultures
| Compound | R | Antiviral activity EC50a (μM) |
Cytotoxicity (μM) | |
|---|---|---|---|---|
| TK+ VZV strain | TK− VZV strain | Cell morphology MCCb | ||
| cis-9a |  |
|||
| (exp. 1) | 20 | 38 | >100 | |
| (exp. 2) | 32 | 45 | >100 | |
| trans-9a | ||||
| (exp. 1) | 32 | 40 | >100 | |
| (exp. 2) | 28 | 41 | >100 | |
| cis-9b |  |
|||
| (exp. 1) | 20 | 38 | >100 | |
| (exp. 2) | 32 | 45 | >100 | |
| trans-9b | ||||
| (exp. 1) | 32 | 40 | >100 | |
| (exp. 2) | 28 | 41 | >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) | >20 | 20 | 100 | |
| (exp. 2) | 11 | 20 | 100 | |
| trans-9d | ||||
| (exp. 1) | 14 | 26 | >100 | |
| (exp. 2) | 15 | 34 | >100 | |
| cis-9e |  |
|||
| (exp. 1) | >20 | 36 | >100 | |
| (exp. 2) | 41 | 44 | >100 | |
| trans-9e | ||||
| (exp. 1) | 30 | 32 | 100 | |
| (exp. 2) | >20 | >20 | 100 | |
| cis-9f |  |
|||
| (exp. 1) | >20 | >20 | 100 | |
| (exp. 2) | >20 | 79 | >100 | |
| trans-9f | ||||
| (exp. 1) | >20 | >20 | 100 | |
| (exp. 2) | >20 | >20 | 100 | |
| Acyclovir | ||||
| (exp. 1) | 3.6 | 44 | >440 | |
| (exp. 2) | 1.5 | 33 | >440 | |
| Brivudin | ||||
| (exp. 1) | 0.042 | 1.0 | >300 | |
| (exp. 2) | 0.029 | 4.9 | >300 | |
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.