Table 2.
Cytotoxicity and Antiviral Activity of Thiosemicarbazides (I and II) and thiosemicarbazones (Ia – Ig and IIa – IIg) in HEL, HeLa and Vero Cell Cultures
| Compound | HEL cell culture | HeLa cell culture | Vero cell culture | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| MCCa) (μg/mL) | EC50b) (μg/mL) | MCCa) (μg/mL) | EC50b) (μg/mL) | MCCa) (μg/mL) | EC50b) (μg/mL) | |||||||||||
| Herpes simpex virus-1 (KOS) | Herpes simplex virus-2 (G) | Vaccina virus | Vesicular stomatitis virus | Herpes simplex virus-1 TK KOS ACVr | Vesicular stomatitis virus | Coxsackie virus B4 | Respiratory syncytical virus | Para influenza-3 virus | Reo virus-1 | Sindbis virus | Coxsackie virus B4 | Punta Toro virus | ||||
| I | >100 | >100 | >100 | 50 | >100 | >100 | ≥100 | >100 | >100 | >100 | 100 | >20 | >20 | >20 | >20 | >20 |
| Ia | >100 | >100 | >100 | >100 | >100 | >100 | ≥100 | >100 | >100 | >100 | >100 | >100 | >100 | >100 | >100 | >100 |
| Ib | 100 | >20 | >20 | >20 | >20 | >20 | 100 | >20 | >20 | >20 | 100 | >20 | >20 | >20 | >20 | >20 |
| Ic | >100 | >100 | >100 | >100 | >100 | >100 | 100 | >20 | >20 | >20 | 100 | >20 | >20 | >20 | >20 | >20 |
| Id | >100 | >100 | >100 | >100 | >100 | >100 | 100 | >20 | >20 | >20 | 100 | >20 | >20 | >20 | >20 | >20 |
| Ie | >100 | >100 | >100 | >100 | >100 | >100 | ≥100 | >100 | >100 | >100 | 100 | >20 | >20 | >20 | >20 | >20 |
| If | >100 | >100 | >100 | >100 | >100 | >100 | ≥100 | >100 | >100 | >100 | >100 | >100 | >100 | >100 | >100 | >100 |
| Ig | >100 | >100 | >100 | >100 | >100 | >100 | ≥20 | >20 | >20 | >20 | >20 | >4 | >4 | >4 | 3 | >4 |
| II | >100 | >100 | >100 | 45 | >100 | 100 | 100 | >20 | >20 | >20 | 100 | >20 | >20 | >20 | >20 | >20 |
| IIa | 100 | >20 | >20 | >20 | >20 | >20 | 100 | >20 | >20 | >20 | 100 | >20 | >20 | >20 | >20 | >20 |
| IIb | >100 | >100 | >100 | >100 | >100 | >100 | >100 | >100 | >100 | >100 | >100 | >100 | >100 | >100 | >100 | >100 |
| IIc | >100 | >100 | >100 | >100 | >100 | >100 | 100 | >20 | >20 | >20 | 100 | >20 | >20 | >20 | >20 | >20 |
| IId | 100 | >20 | >20 | >20 | >20 | >20 | >100 | >100 | >100 | >100 | 100 | >20 | >20 | >20 | >20 | >20 |
| IIe | 100 | >20 | >20 | >20 | >20 | >20 | >100 | >100 | >100 | >100 | 100 | >20 | >20 | >20 | >20 | >20 |
| IIf | >100 | >100 | >100 | >100 | >100 | >100 | 100 | >20 | >20 | >20 | 100 | >20 | >20 | >20 | >20 | >20 |
| IIg | 100 | >20 | >20 | >20 | >20 | >20 | ≥100 | >100 | >100 | >100 | 100 | >20 | >20 | >20 | >20 | >20 |
| Brivudin (μM) | >250 | 0.04 | 100 | 10 | >250 | 100 | ||||||||||
| Cidofovir (μM) | >250 | 2 | 2 | 29 | >250 | 2 | ||||||||||
| Acyclovir (μM) | >250 | 0.4 | 0.2 | >250 | >250 | 112 | ||||||||||
| Ganciclovir (μM) | >100 | 0.03 | 0.06 | >100 | >100 | 10 | ||||||||||
| DS-5000c) | >100 | 2 | 34 | 0.6 | >100 | >100 | >100 | 100 | 9 | 100 | ||||||
| (S)-DHPAd) (μM) | >250 | >250 | >250 | >250 | >250 | >250 | >250 | >250 | >250 | >250 | ||||||
| Ribavirin (μM) | >250 | 5 | 112 | 10 | >250 | 112 | >250 | >250 | >250 | 146 | ||||||
a) Required to cause a microscopically detectable alteration of normal cell morphology.
b) Required to reduce virus-induced cytopathogenicity by 50%.
c) DS-5000: dextran sulfate (molecular weight, 5.000).
d) (S)-DHPA: (S)-9-(2,3-dihydroxypropyl)adenine.