Table 5.
Antiviral activity of thiourea derivatives against HIV-1 and ssRNA+ (BVDV, YFV, CV-B5, Sb-1) viruses and cytotoxicity against the cell lines used in the assays.
| Compounds | MT-4 a CC50 | HIV-1 b EC50 | MDBK c CC50 | BVDV d EC50 | BHK e CC50 | YFV f EC50 | Vero-76 g CC50 | CV-B5 h EC50 | Sb-1 i EC50 |
|---|---|---|---|---|---|---|---|---|---|
| 1 | 31 | >31 | >100 | >100 | 48 | >48 | 64 | >64 | >64 |
| 2 | 32 | >32 | >100 | >100 | 44 | >44 | 56 | >56 | >56 |
| 3 | 33 | >33 | >100 | ≥100 | 16 | >16 | 75 | >75 | >75 |
| 4 | 45 | >45 | >100 | >100 | 47 | >47 | 55 | >55 | >55 |
| 5 | 38 | >38 | 67 | 20 ± 1.5 | 34 | >34 | 29 | >29 | >29 |
| 6 | 45 | >45 | 27 | >27 | 10 | >10 | 13 | >13 | >13 |
| 7 | 45 | >45 | 55 | 20 ± 2.0 | 10 | >10 | 12 | >12 | >12 |
| 8 | 45 | 8.7 ± 0.4 | 52 | >52 | 10 | >10 | 13 | >13 | >13 |
| 9 | 49 | >49 | 55 | >55 | 13 | >13 | 14 | >14 | >14 |
| 10 | 78 | >78 | >100 | >100 | 52 | >52 | >100 | 30 ± 2.4 | >100 |
| 11 | 48 | >48 | 69 | >69 | 34 | >34 | 73 | >73 | >73 |
| 12 | 47 | >47 | 49 | >49 | 16 | >16 | 60 | >60 | >60 |
| 13 | 47 | >47 | 49 | >49 | 11 | >11 | 53 | 12 ± 0.9 | >53 |
| 14 | 42 | >42 | 32 | >32 | 6.0 | >6.0 | 32 | 9.0 ± 1.2 | >32 |
| 15 | 46 | >46 | 48 | >48 | 28 | >28 | 46 | >46 | >46 |
| 16 | 49 | >49 | >100 | 46 | 18 | >18 | >100 | 18 ± 1.7 | >100 |
| 17 | 44 | >44 | 53 | >53 | 30 | >30 | 53 | >53 | >53 |
| 18 | >100 | >100 | >100 | >100 | >100 | >100 | >100 | >100 | >100 |
| 19 | >100 | >100 | >100 | ≥100 | 35 | >35 | 89 | >89 | >89 |
| 20 | >100 | >100 | >100 | 35 ± 2.8 | >100 | >100 | >100 | >100 | >100 |
| 21 | 2.4 ± 0.2 | >2.4 | >100 | >100 | 11 | >11 | 11 | >11 | >11 |
| 22 | >100 | >100 | >100 | >100 | >100 | >100 | >100 | >100 | >100 |
| 23 | 44 | >44 | 25 | >25 | 10 | >10 | 17 | >17 | >17 |
| 24 | 44 | >44 | 23 | >23 | 9.0 | >9.0 | 16 | >16 | >16 |
| 25 | >100 | >100 | >100 | >100 | >100 | >100 | >100 | >100 | >100 |
| 26 | 45 | >45 | 42 | 15 ± 1.2 | 12 | >12 | 17 | >17 | >17 |
| 27 | 45 | >45 | 11 | >11 | 9.5 | >9.5 | 12 | >12 | >12 |
| 28 | 45 | >45 | 37 | 13 ± 1.2 | 30 | >30 | 32 | 20 ± 2.1 | >32 |
| Efavirenz | 40 | 0.002 ± 0.0002 | |||||||
| 2′-C-methyl-guanosine | >10 | 1.1 ± 0.1 | >10 | 1.9 ± 0.1 | |||||
| 2′-C-methyl-cytidine | >100 | 18 ± 0.9 | 7.3 ± 0.4 | ||||||
Data represent mean values for three independent determinations. Standard deviations are reported for the more active compounds. Also for the others values the variation was less than 15%. a Compound concentration (µM) required to reduce the proliferation of mock-infected MT-4 cells by 50%. b Compound concentration (µM) required to achieve 50% protection of MT-4 cells from HIV-1 induced cytopathogenicity. c Compound concentration (µM) required to reduce the viability of mock-infected MDBK cells by 50%. d Compound concentration (µM) required to achieve 50% protection of MDBK cells from BVDV-induced cytopathogenicity. e Compound concentration (µM) required to reduce the viability of mock-infected BHK cells by 50%. f Compound concentration (µM) required to achieve 50% protection of BHK cells from YFV-induced cytopathogenicity. g Compound concentration (µM) required to reduce the viability of mock-infected VERO-76 cells by 50%. h,i Compound concentration (µM) required to reduce the plaque number of CV-B5 h, Sb-1 i by 50% in VERO-76 monolayers.