TABLE 2.
Anti-HIV-1(IIIB) activity of test compounds in CEM, C8166, MT-2, and MT-4 cellsa
| Compound | CEM
|
C8166
|
MT-2
|
MT-4
|
||||
|---|---|---|---|---|---|---|---|---|
| EC50 | CC50 | EC50 | CC50 | EC50 | CC50 | EC50 | CC50 | |
| JPL-10 | 5.3 ± 2.6 | 31 ± 6 | 6.1 ± 1.5 | 9.8 ± 3.2 | 8.0 ± 1.3 | 8.0 ± 3.1 | 7.9 ± 1.7 | 34 ± 1 |
| JPL-27 | 6.8 ± 3.5 | 29 ± 6 | 7.0 ± 4.1 | 29 ± 1 | 16 ± 3 | 26 ± 1 | 17 ± 4 | 30 ± 12 |
| JPL-30 | 5.9 ± 3.0 | 70 ± 20 | 5.7 ± 2.5 | 59 ± 16 | 12 ± 2 | 26 ± 3 | 9.1 ± 3.4 | ≥100 |
| JPL-71 | 0.10 ± 0.01 | 36 ± 3 | 0.10 ± 0.04 | 1.7 ± 0.4 | 0.20 ± 0.10 | 11 ± 1 | 0.12 ± 0.01 | 11 ± 2 |
| JPL-74 | 0.48 ± 0.01 | >4b | 0.40 ± 0.11 | 1.4 ± 0.2 | 0.64 ± 0.23 | >4b | 1.3 ± 0.2 | >4b |
| JPL-78 | 3.4 ± 0.9 | >100 | 5.0 ± 2.9 | 6.9 ± 3.2 | 8.6 ± 2.0 | >100 | 2.4 ± 0.1 | 60 ± 30 |
| JPL-107 | 0.52 ± 0.03 | >4b | 1.0 ± 0.4 | 1.6 ± 0.3 | 1.3 ± 0.5 | >4b | 0.54 ± 0.05 | >4b |
| JPL-110 | 9.6 ± 1.4 | ≥100 | ≥4 | 2.8 ± 0.1 | 23 ± 11 | 34 ± 14 | 11 ± 5 | 26 ± 10 |
| JPL-133 | 0.05 ± 0.01 | 38 ± 6 | 0.04 ± 0.01 | 6.2 ± 0.7 | 0.10 ± 0.03 | 16 ± 7 | 0.12 ± 0.01 | 13 ± 2 |
| JPL-146 | 2.2 ± 0.2 | 30 ± 7 | 2.8 ± 0.8 | 29 ± 10 | 2.4 ± 0.8 | 21 ± 4 | 2.8 ± 0.8 | 28 ± 12 |
| JPL-150 | 4.0 ± 0.1 | 42 ± 10 | 4.0 ± 0.9 | 30 ± 5 | 8.8 ± 2.0 | 28 ± 8 | 8.1 ± 3.2 | 46 ± 7 |
a
EC50, compound concentration required to inhibit HIV-1-induced cytopathicity (giant cell formation) in CEM, C8166, and MT-2 cells or HIV-induced cytopathicity (cell lysis) in MT-4 cells by 50%; CC50, compound concentration required to reduce cell viability (MT-4) or to inhibit cell proliferation (CEM, C8166, and MT-2) by 50%. Data represent the average values (± standard deviation) for at least three independent experiments.
b
Higher drug concentrations could not be accurately determined due to insolubility of the compound at these concentrations.