Table 1.
Antiviral effects and cytotoxicity of S-PMEA 3 and S-PMPA 4 and reference compounds PMEA and PMPA, in CEM cells infected by 100 TCID50 of HIV-1(IIIa) or HIV-2(ROD), in H9 cells infected by 125 and 6250 TCID50 of HIV-1-LAI and in activated PBMC infected by 100 TCID50 of HIV-1-LAI.
Compounds | CEM |
H9 |
PBMC |
PBMC and H9 |
|||
---|---|---|---|---|---|---|---|
EC50 (μM)a 100 TCID50 HIV-1(IIIB) |
EC50 (μM)a 100 TCID50 HIV-2(ROD) |
CC50 (μM)b | EC50 (μM)a 125 TCID50 HIV-1-LAI |
EC50 (μM)a 6250 TCID50 HIV-1-LAI |
EC50 (μM)a 100 TCID50 HIV-1-LAI |
CC50 (μM)b | |
S-PMEA 3 | 16 ± 3.4 | 23 ± 19 | 233 ± 5.3 | 1.9 ± 1.8 | 17 ± 0.8 | 14 ± 10 | >30 |
PMEA | 5.5 ± 1.7 | 7.0 ± 4.3 | 85 ± 19 | 1.1 ± 0.7 | 7.9 ± 4.2 | 3.2 ± 2.1 | >30 |
S-PMPA 4 | 14 ± 1.6 | 7.9 ± 3.0 | >250 | 0.38 ± 0.10 | 9.7 ± 0.1 | 4.2 ± 3.9 | >100 |
PMPA | 4.1 ± 1.0 | 7.1 ± 5.7 | >250 | 0.23 ± 0.05 | 8.3 ± 1.7 | 3.4 ± 3.2 | >100 |
CEM: HumanT-Lymphoblastoid cells; H9: human lymphocyte cells; PMBC: Peripheral blood mononuclear cells.
EC50 or concentration of drug that decreases the HIV replication by 50% (means of EC50 from two blood donors).
CC50 or concentration of drug that reduces the viable cell number by 50% (means of CC50 from two blood donors).