Table 1.
Antiretroviral activity, cell toxicity, and therapeutic indices for triterpene derivatives.
| Triterpene derivative | Antiretroviral activity (treatment of virus-producing cells) | Antiretroviral activity (treatment of permissive target cells) | Cell toxicity | Therapeutic indexc |
|---|---|---|---|---|
| EC50, μMa | EC50, μMb | IC50, μMb | ||
| Bevirimat | 0.28 (±0.09) | >50 | >300 | >1000 |
| 4 | 15 (±2.5) | >50 | >150 | >10 |
| 7 | 1.5 (±0.4) | >50 | >300 | >200 |
| 9 | 14 (±2.7) | >50 | >130 | >9.2 |
| 15 | 39 (±10) | >50 | >300 | >7.6 |
| 18 | 1.8 (±0.5) | >50 | >300 | >160 |
| 19 | 1.2 (±0.3) | >50 | >300 | >250 |
| 20 | 1.5 (±0.5) | >50 | 29 | 19 |
| 21 | 1.4 (±0.4) | >50 | >300 | >210 |
a
Mean of four experiments, standard deviation is given in parentheses.
b
Mean of three experiments.
c
Therapeutic index = IC50 cytotoxicity/EC50 antiretroviral activity.