TABLE 3.
Antiretroviral activity of BDM-2 and two representative analogs on cultures of primary T CD4+ lymphocytes infected with lab-adapted and clinical HIV-1 isolates
| Compound | Infection assays in primary T CD4+ lymphocytes: EC50 (nM)a |
|||||
|---|---|---|---|---|---|---|
| NL4-3 | HXB2 | KER2008 | 33913N | NP1538 | NP1525 | |
| (B) | (B) | (A) | (B) | (B) | (CRF01_AE) | |
| RAL | 4.9 ± 2.3 | 2.6 ± 1.4 | 6.7 ± 4.0 | 2.1 ± 0.1 | 1.7 ± 1.9 | 4.0 ± 1.7 |
| DTG | 0.53 ± 0.16 | 0.17 ± 0.01 | 0.40 ± 0.21 | 0.35 ± 0.42 | 0.29 ± 0.13 | 0.21 ± 0.09 |
| BI-224436 | 100 ± 80 | 14 ± 7 | 37 ± 12 | 20 ± 9 | 66 ± 42 | 61 ± 35 |
| S-I-82 | 9.9 ± 1.1 | 5.2 ± 3.9 | 11 ± 2 | 4.4 ± 1.9 | 8.6 ± 0.5 | 10 ± 4 |
| BDM-2 | 8.3 ± 4.3 | 3.4 ± 1.0 | 8.1 ± 1.3 | 4.2 ± 1.6 | 13 ± 6 | 11 ± 5 |
| MUT871 | 2.8 ± 0.5 | 1.8 ± 0.3 | 6.4 ± 1.3 | 1.5 ± 0.6 | 4.0 ± 2.3 | 3.5 ± 0.6 |
| MUT884 | 15 ± 4 | 10 ± 6 | 19 ± 3 | 5.8 ± 3.2 | 41 ± 2 | 12 ± 3 |
a
EC50 values are reported for multiple-round infection assays for each HIV-1 strain (clade indicated in parenthesis). Two INSTIs (RAL, DTG) and two INLAIs (BI-224436, S-I-82) were used as references. Data are mean ± SD of n > 5 independent experiments.