Table 1.
Anti-HIV and cellular toxicity evaluation of CXCR4 antagonists.
| Compound | Anti-HIV Activity a IC50 (nM) |
Toxicity b CC50 (µM) |
|
|---|---|---|---|
| NL4-3 (X4) | BaL (R5) | PMBCs | |
| Cu2L1 | 10.1 ± 1.6 | >20,000 | >100 |
| Zn2L1 | 0.73 ± 0.34 | >15,000 | >90 |
| Cu2L2 | 12.9 ± 2.8 | >20,000 | >100 |
| Zn2L2 | 2.9 ± 1.2 | >15,000 | >100 |
| Cu2L3 | 0.74 ± 0.60 | >5000 | >40 |
| Zn2L3 | 6.2 ± 2.5 | >1000 | >100 |
| Cu2L4 | 0.87 ± 0.32 | >2000 | >10 |
| Zn2L4 | 4.8 ± 1.5 | >2000 | >90 |
| Cu2L5 | 31.6 ± 2.4 | >20,000 | >30 |
| Zn2L5 | 16.9 ± 0.9 | >20,000 | >100 |
| AMD3100 | 0.42 ± 0.14 | >20,000 | >100 |
| Maraviroc | >20,000 | 2.9 ± 1.2 | >100 |
a Concentration required to inhibit the replication of the HIV-1 strains NL4-3 (X4) and BaL (R5) in TZM-bl cells by 50%. b Concentration required to reduce cell (PMBCs) viability by 50%. Data are presented as the mean ± SEM of two to five experiments.