Table 3.
Cytotoxicity against MT-4, MDBK, BHK and Vero-76 cell lines and BVDV, YFV, Reo-1, CVB-2, RSV and HSV-1 inhibitory activity of amino azocompounds of structure A–C
| Compda | R | MT-4 CC50b | MDBK CC50c | BVDV EC50d | BHK-21 CC50e | YFV EC50f | Reo-1 EC50g | VERO-76 CC50h | CVB-2 EC50i | RSV EC50j | HSV-1 EC50k |
|---|---|---|---|---|---|---|---|---|---|---|---|
| 1 | H | 17 | 58 | 1.6 | 31 | ⩾31 | >31 | 30 | >30 | 25 | >30 |
| 2l | 3-NO2 | 14 | 33 | 16 | 20 | 7 | >20 | 25 | 11 | >25 | 6 |
| 3 | 4-NO2 | 19 | >100 | >100 | >100 | >100 | >100 | 60 | >60 | >60 | >60 |
| 4l | 2,5-diF | 16 | 59 | 9 | 33 | 12 | >33 | 30 | >30 | >30 | 12 |
| 5 | 2,6-diF | 35 | 20 | ⩾20 | 43 | 10 | 12 | 65 | >65 | >65 | >65 |
| 6 | 4-CH3 | 17 | >100 | >100 | >100 | >100 | >100 | 50 | >50 | >50 | >50 |
| 7 | H | 31 | 48 | 2.5 | 47 | 9 | >47 | 60 | >60 | >60 | >60 |
| 8 | 3-CF3 | 77 | 52 | 7 | ⩾100 | >100 | >100 | 80 | >80 | >80 | >80 |
| 9 | H | 100 | >100 | 30 | >100 | ⩾100 | >100 | 80 | >80 | >80 | >80 |
| 10 | 3-CF3 | 15 | 30 | 7 | 14 | >14 | >14 | 50 | >50 | >50 | >50 |
| 11 | 2,5-diF | 40 | 64 | >64 | 38 | >38 | >38 | 80 | >80 | >80 | >80 |
| 12 | 2,4-diF | 51 | 11 | >11 | 9 | >9 | >9 | 15 | >15 | >15 | >15 |
| NM 108 (2′-C-methylguanosine) | >100 | >100 | 1.7 | 90 | 1.8 | 2.4 | >100 | 20 | >100 | >100 | |
| NM 299 (6-azauridine) | 2 | >100 | >100 | >100 | 26 | >100 | 20 | >20 | 1.2 | >20 | |
| ACG (acycloguanosine) | >100 | >100 | >100 | >100 | >100 | >100 | >100 | >100 | >100 | 3 | |
| Ribavirin | 31 | >100 | 7 | >100 | >100 | >100 | >100 | >100 | 7 | >100 | |
| NM 176 (2′-C-ethynylcytidine) | ⩾100 | >100 | 38 | >100 | >100 | >100 | >100 | 24 | >100 | >100 | |
| M 5255 (mycophenolic acid) | 0.2 | 42 | >42 | >100 | >100 | >100 | ⩾13 | >13 | 0.6 | >13 | |
None of these compounds inhibited the multiplication of HIV-1, VSV, VV and Sb-1 viruses.
Compound concentration (μM) required to reduce the viability of mock-infected MT-4 (CD4+ human T cells containing an integrated HTLV-1 genome) cells by 50%, as determined by the MTT method.
Compound concentration (μM) required to reduce the viability of mock-infected MDBK (Bovine normal kidney) cells by 50%, as determined by the MTT method.
Compound concentration (μM) required to achieve 50% protection of MDBK cells from BVDV (Bovine Viral Diarrhea Virus) induced cytopathogenicity, as determined by the MTT method.
Compound concentration (μM) required to reduce the viability of mock-infected BHK (Hamster normal kidney fibroblast) monolayers by 50%, as determined by the MTT method.
Compound concentration (μM) required to achieve 50% protection of BHK cells (kidney fibroblast) from YFV (Yellow Fever Virus) induced cytopathogenicity, as determined by the MTT method.
Compound concentration (μM) required to achieve 50% protection of BHK cells (kidney fibroblast) from Reo-1 induced cytopathogenicity, as determined by the MTT method.
Compound concentration (μM) required to reduce the viability of mock-infected VERO-76 (monkey normal kidney) monolayers by 50%.
Compound concentration (μM) required to reduce the plaque number of CVB-2 (Coxsackie Virus B 2) by 50% in VERO-76 monolayers.
Compound concentration (μM) required to reduce the plaque number of RSV (Respiratory Syncytial Virus) by 50% in VERO-76 monolayers.
Compound concentration (μM) required to reduce the plaque number of HSV-1 (Herpes Simplex virus, Type-1) by 50% in VERO-76 monolayers.
Tested as hydrochloride.