Table 2.
Biological activity of (dehydro)epiandrosterone derivatives.
| Compound | % Cytotoxicity (50 µM) a | EC50 (µM) a | CC50 (µM) a | Selectivity Index b |
|---|---|---|---|---|
|
T. Cruzi Epimastigote Form |
T. brucei Bloodstream Form |
Murine Macrophage (Cell Line J774) |
||
| EA | 3.7 ± 0.7 | 36.5 ± 3.6 c | >100 | >2.7 |
| 1 | 14.5 ± 5.3 | 1.9 ± 0.2 | 8.8 ± 1.0 | 4.6 |
| 2 | 64.0 ± 4.1 | 5.3 ± 0.4 | 42.0 ± 1.0 | 7.9 |
| 3 | 73.9 ± 3.4 | 4.8 ± 0.5 | 1.0 ± 0.1 | 0.2 |
| DHEA | n.d. | 43.8 ± 2.0 c | 25.0 ± 13.0 d | 0.6 |
| 4 | 6.4 ± 1.6 | 7.5 ± 0.3 | 19.0 ± 3.0 | 2.5 |
| 5 | 30.9 ± 2.5 | 18.0 ± 3.0 | 39.0 ± 3.0 | 2.2 |
| 6 | 76.2 ± 0.8 | 5.3 ± 0.5 | 4.5 ± 0.4 | 0.9 |
| 7 | 3.9 ± 0.7 | >24 | >24 | n.d |
| Conessine | n.d. | 0.42 ± 0.01 e | 61.2 e | 145.7 |
| Nifurtimox | 46.0 ± 1.9 (at 24 µM) | 6.0 ± 0.4 | 140.0 ± 2.0 | 23.3 |
a Data presented as mean value ± standard deviation of at least three independent determinations. b The selectivity index (SI) was calculated as the ratio: CC50 for murine macrophages/EC50 for T. brucei. c value reported by [44]. d value reported against Hek293T by [27]. e Values against mammalian L6 cell line from rat skeletal myoblasts reported by [44]. n.d. not determined.