Table 6.
Antiviral activity against varicella-zoster virus and human cytomegalovirus.
| Cpd. | VZV TK+ (OKA) EC50a (μM) | VZV TK− (07_01) EC50a (μM) | MCCb (μM) | CC50c (μM) | CMV (AD-169) EC50d (μM) | CMV (Davis) EC50d (μM) | MCCe (μM) | CC50f (μM) | |
|---|---|---|---|---|---|---|---|---|---|
| 5 | 1.82 ± 0.24 | 1.64 ± 0.44 | 20 | 0.7 ± 0.1 | ≥4 | ≥4 | 20 | 0.73 ± 0.07 | |
| 59 | 1.71 ± 0.63 | 3.74 ± 2.69 | ≥20 | 3.41 ± 2.25 | 1.79 | >4 | 4 | N.D. | |
| 66 | 16.55 | 3.06 | 20 | N.D. | 0.51 ± 0.0 | 0.53 ± 0.09 | ≥20 | 5.25 ± 3.80 | |
| 67 | 2.76 ± 0.09 | 2.27 ± 1.74 | ≥100 | 0.35 ± 0.02 | 0.36 ± 0.0 | 0.35 ± 0.02 | >100 | 0.35 ± 0.02 | |
| 68 | 9.82 ± 2.21 | 8.26 ± 2.74 | 20 | 0.16 ± 0.0 | 2.31 ± 1.70 | 0.66 ± 0.15 | 20 | 0.16 ± 0.0 | |
| 70 | >100 | >100 | >100 | N.D. | >100 | >100 | 20 | N.D. | |
| 80 | >100 | 17.49 | >100 | N.D. | >100 | 20 | 100 | N.D. | |
| Acyclovir | 1.26 ± 0.73 | 36.74 ± 2.95 | >440 | >440 | N.D. | N.D. | N.D. | N.D. | |
| Cidofovir | N.D. | N.D. | N.D. | N.D. | 1.59 ± 0.35 | 1.45 ± 0.18 | >300 | N.D. | |
| Ganciclovir | N.D. | N.D. | N.D. | N.D. | 11.75 ± 0.32 | 6.52 ± 0.53 | >350 | N.D. | |
aActivity against varicella-zoster virus (VZV) in Hel (human embryonic lung) culture; TK−: thymidylate kinase knock-out strain; EC50 values (μM) represent the concentration of compound that reduces virus-induced cytopathicity by 50%.b,e MCC or minimal cytotoxic concentration represents the concentration of test compound that causes a microscopically detectable alteration of normal cell morphology.c,f CC50 represents the concentration (μM) of test compound that reduces cell (Hel) proliferation by 50% as determined by Coulter Counter.d Antiviral activity against cytomegalovirus (CMV) in Hel culture; EC50 values (μM) represent the concentration of compound that reduce virus-induced cytophathicity by 50%.