IC50 | CC50 | ||||
---|---|---|---|---|---|
CD4 Down-Modulation | Anti-HIV-1 | Toxicity | |||
Compound | MT-4 | SupT1 | MT-4 | MT-4 | SupT1 |
μM | μM | ||||
CADA | 0.80 ± 0.35 | 1.03 ± 0.21 | 1.21 ± 0.07 | 40.7 ± 5.4 | >75 |
QJ023 | 0.57 ± 0.27 | 0.68 ± 0.16 | 0.60 ± 0.19 | 32.7 ± 6.4 | 40.4 ± 10.7 |
QJ027 | 7.86 ± 1.55 | 10.49 ± 0.13 | 8.02 ± 0.43 | 35.3 ± 3.3 | 37.0 ± 3.0 |
QJ028 | 0.34 ± 0.06 | 0.43 ± 0.07 | 0.29 ± 0.05 | 29.3 ± 7.8 | 36.4 ± 23.9 |
QJ029 | 4.08 ± 0.82 | 5.80 ± 1.04 | 2.39 ± 1.59 | 36.4 ± 4.3 | 37.9 ± 3.1 |
QJ030 | 5.46 ± 2.06 | 11.12 ± 3.64 | 6.13 ± 2.20 | 32.4 ± 1.4 | >75 |
QJ033 | 2.12 ± 0.26 | 4.18 ± 1.13 | 2.60 ± 0.69 | 44.1 ± 1.2 | >75 |
QJ035 | 11.00 ± 1.50 | >15 | 10.59 ± 1.22 | 38.9 ± 1.9 | 40.4 ± 0.9 |
QJ036 | 3.04 ± 1.57 | 3.48 ± 0.55 | 3.52 ± 1.91 | 42.6 ± 6.3 | >75 |
QJ037 | 0.98 ± 0.16 | 1.34 ± 0.34 | 0.98 ± 0.25 | 34.5 ± 7.8 | 43.1 ± 10.9 |
QJ038 | 0.67 ± 0.09 | 0.96 ± 0.33 | 0.77 ± 0.35 | 32.5 ± 1.6 | 13.1 ± 5.1 |
QJ040 | 8.29 ± 1.21 | 13.06 ± 1.51 | 6.39 ± 1.00 | 30.3 ± 4.4 | 34.1 ± 4.1 |
QJ041 | 6.57 ± 2.87 | 7.36 ± 0.91 | 6.62 ± 0.47 | 36.1 ± 8.5 | 36.6 ± 2.8 |
AS-N6P6 | 5.44 ± 1.43 | 5.76 ± 1.42 | 5.60 ± 2.79 | 32.6 ± 11.9 | >75 |
95–213 | 11.09 ± 0.69 | 16.15 ± 2.14 | 27.15 ± 18.20 | >75 | >75 |
98–035 | 10.33 ± 3.33 | 10.93 ± 1.88 | 19.30 ± 14.86 | >75 | >75 |
HJC321 | 3.65 ± 1.73 | 4.95 ± 0.32 | 7.31 ± 1.72 | 41.0 ± 1.0 | >75 |
AS117 | 1.90 ± 0.48 | 2.26 ± 0.25 | 2.20 ± 0.63 | 46.9 ± 9.7 | >75 |
AS-PB127 | 1.76 ± 0.26 | 3.78 ± 2.60 | 1.84 ± 0.04 | 47.7 ± 13.2 | >75 |
95–210 | 10.94 ± 2.93 | >75 | >15 | 38.0 ± 2.5 | >75 |
98–037 | >75 | >75 | >75 | >75 | >75 |
AS112 | >15 | >75 | >15 | 43.0 ± 1.4 | >75 |
97–269 | >75 | >75 | >75 | >75 | >75 |
MFS010 | >15 | >75 | >15 | 47.2 ± 6.7 | >75 |
MFS117 | >15 | >75 | >15 | 30.5 ± 11.6 | >75 |
MFS105 | >75 | >75 | >75 | >75 | >75 |
95–211 | >15 | >75 | >15 | 40.2 ± 1.9 | >75 |
MFS-PB001 | >15 | >15 | >15 | 34.3 ± 0.8 | 49.2 ± 12.7 |
The compounds were used in the free base or salt forms as listed underMaterials and Methods. IC50 for CD4 down-modulation was the concentration of the compound required for 50% inhibition of cell surface CD4 expression in MT-4 or SupT1 cells, as measured by flow cytometry. IC50 for HIV-1 (NL4.3) infection in MT-4 cells was concentration of the compound required to reduce viral HIV-1 replication by 50% as measured by the p24 Ag ELISA. CC50 was the 50% cytotoxic concentration (i.e., the concentration of the compound required to reduce the viability of the MT-4 or SupT1 cells by 50%). Data represent mean values ± S.D. for three or four independent experiments.