Table 1. IC50 Cell Free Assays Translation Inhibition Activity of Peptolides against Prokaryotic and Eukaryotic Ribosomal Preparationsa.
| compds. | E. coli IC50 (μM) | rabbit retic. IC50 (μM) |
|---|---|---|
| 12a | 1.32 ± 0.08 | >250 |
| 12b | 0.67 ± 0.28 | >250 |
| 13 | >250b | >250 |
| 12c | 1.86 ± 0.35 | >250 |
| 12d | 1.10 ± 0.22 | >250 |
| 14 | >250b | >250 |
| 12e | 4.32 ± 0.25 | 140 |
| 12f | 2.73 ± 0.82 | 38 |
| 15 | >1000c | 205 |
| 12g | 56.00 ± 9.60 | >250 |
| 12h | 7.41 ± 1.20 | >250 |
| 16 | >250b | >250 |
| TE-802 | 0.52 ± 0.05 | >250 |
| clarithromycin 1 | 0.32 ± 0.12 | >250 |
a
Luciferase activity was used as a reporter of translation inhibition in both systems. IC50 values were obtained from an average of three independent experiments.
b
No inhibition at maximum tested concentration (250 μM).
c
Maximum tested concentration increased 4-fold to obtain information about the extent of selectivity over RRL.