Table 1.
Cytotoxicitya and translation inhibition of psymberin, mycalamide and analogs against human tumor cell lines.b
| Compound | Cytotoxicity (IC50, nM) | Translation Inhibition (EC50, nM)***
|
|||
|---|---|---|---|---|---|
| in vitro assay | cell-based assay | ||||
|
| |||||
| Hela* | SK-MEL-5** | HeLa | SK-MEL-5 | ||
| Cycloheximide | 2242±1515 | 3116±754 | 3150±2152 | 3325±834 | 2670 |
| 1a | 0.64±0.14 | 0.27±0.04 | 28±7 | 2.2±1.4 | 11±10 |
| 1b | 0.54±0.01 | 0.35±0.07 | 142±21 | 5.8±1.7 | 4.2±3.2 |
| 1c | 2.34±0.53 | 1.58±0.42 | 120±47 | 9.6±8.9 | 9.3±8.5 |
| 8 | 2.52±1.39 | 3.79±0.04 | 238±44 | 59±32 | 64 |
| 3 | 618.6±267.0 | 352.0±12.1 | 346±64 | 4950±4870 | 496 |
| 4 | >1000 | 762.8±70.0 | 318±182 | 2200±1410 | 843 |
| 5 | >1000 | >1000 | 641±262 | 1650±1060 | 578 |
| 6 | >1000 | >1000 | >10000 | >10000 | >10000 |
| 7 | >1000 | >1000 | >10000 | >10000 | >10000 |
a
A CellTiter-Glo® luminescent assay, which measures cellular ATP concentrations, was used to measure cell viability with and without compound treatment. IC50 values were calculated by fitting the luminescence data to an equation representing the dose-response of inhibiting luminescence.
b
Data are means ± standard deviation from at least two independent experiments conducted in triplicate.
*
R2 values range from 0.931 to 0.994.
**
R2 values range from 0.865 to 0.997.
***
R2 ranges from 0.90 to 0.995.