Table 6. Hepatocyte Stability, Cytotoxicity, and hERG Inhibition of Selected Compounds.
| compounds | hepatocyte
stability |
cytotoxicity (HepG2) | hERG K+ | |||
|---|---|---|---|---|---|---|
| mouse |
human |
|||||
| t1/2 (min) | %remaininga | t1/2 (min) | %remaininga | IC50 (μg/mL) | IC50 (μM) | |
| 23j | 56.4 | 69.1 | 50.8 | 66.4 | >64 | 23.7 |
| 24f | 43.7 | 62.1 | 38.1 | 58.0 | >64 | >30 |
| 24j | 19.3 | 34.0 | 72.5 | 75.1 | >64 | 28.3 |
| 25a | 27.1 | 46.5 | 20.3 | 35.9 | >64 | 22.6 |
| 25b | 12.5 | 19.0 | 32.6 | 52.8 | >64 | >30 |
| TCA1 | 85.3 | 74.8 | 5.97 | 3.1 | 46.1 | 18.3 |
a
Substrate concentrations were determined in incubations after 30 min and normalized to concentrations at time zero.