Anti-HIV-1 activity of the different bicyclam analogues and the CXC-chemokine SDF-1α
| Compound | EC502-a(μg/ml) | CC502-b (μg/ml) | |||||
|---|---|---|---|---|---|---|---|
| NL4-3 | AOM | RF | 168.102-c | BaL2-d | AMD3100-resistant NL4-3 | ||
| AMD2763 | 0.35 | 0.19 | 1.26 | 0.2 | >25 | >25 | >250 |
| AMD3068 | 0.134 | 0.65 | 0.07 | 0.02 | NT2-e | 3.00 | >250 |
| AMD3070 | 0.090 | 0.067 | 0.08 | 0.02 | 15 | 0.48 | >250 |
| AMD3100 | 0.005 | 0.05 | 0.13 | 0.002 | >25 | 0.41 | >250 |
| AMD3109 | 0.100 | 0.05 | 0.08 | 0.24 | >25 | 5.00 | >250 |
| AMD3120 | 7.18 | 86.7 | >250 | 6.0 | >25 | >50 | >250 |
| AMD3128 | 0.20 | 0.22 | 0.36 | 0.24 | >25 | >25 | >250 |
| AMD3158 | 25.8 | 23.4 | 125 | 2.0 | NT | >100 | >250 |
| AMD3166 | 0.036 | 0.086 | 0.12 | 0.048 | NT | 0.68 | >250 |
| AMD3196 | 0.134 | 0.34 | 0.39 | 0.24 | >25 | 12.10 | >250 |
| AMD3203 | 0.20 | 0.08 | 0.1 | 0.12 | NT | 0.42 | >250 |
| AMD3207 | 0.020 | 0.03 | 0.07 | 0.01 | NT | 0.24 | 185 |
| AMD3208 | >250 | >10.0 | >10 | NT | NT | >250 | >250 |
| AMD3209 | 0.81 | 0.87 | 1.4 | 1.2 | NT | >25 | >250 |
| AMD3390 | 30.4 | 5.6 | >250 | 1.2 | NT | >5 | >250 |
| AMD3461 | 11.1 | 7.98 | >250 | 6.0 | NT | >50 | >250 |
| AMD3462 | 0.008 | 0.028 | 0.08 | 0.048 | NT | 0.26 | >250 |
| AMD3469 | 0.023 | 0.074 | 0.27 | NT | NT | >1 | >250 |
| AMD3479 | 0.007 | 0.015 | 0.023 | <0.08 | 7 | 0.30 | >250 |
| AMD6037 | 0.20 | 0.56 | 1.94 | 0.24 | >25 | >25 | >250 |
| AMD6038 | 0.04 | 0.14 | 0.22 | 0.04 | >25 | 2.65 | >250 |
| SDF-1α | 0.30 | 1.06 | 1.36 | 0.2 | NT | >2.00 | >5 |
↵2-a EC50 as measured by the MTT assay.
↵2-b CC50: 50% cytotoxic concentration, or concentration of the compound required to reduce the viability of MT-4 cells by 50%, as measured by the MTT assay.
↵2-c EC50 in SUP-T1 cells.
↵2-d EC50 based on the inhibition of HIV-1-induced β-galactosidase activity in MAGI-CD4-CCR5 cells.
↵2-e NT, not tested.