Table 1.
Antiproliferative activity of ent-kauranic derivatives. DT–docetaxel; SP–staurosporine.
| Compound | Conc. Unit | IC50 | |||||||
|---|---|---|---|---|---|---|---|---|---|
| hTERT RPE-1 | Capan-1 | HCT-116 | NCI-H460 | DND-41 | HL-60 | K-562 | Z-138 | ||
| 7 | µM | 29.2 ± 1.2 | 37.1 ± 3.9 | 30.7 ± 16.4 | 12.0 ± 1.5 | 36.5 ± 0.7 | 19.6 ± 7.7 | 24.7 ± 11.8 | 27.6 ± 15.5 |
| 11 | µM | 1.8 ± 0.4 | 1.7 ± 0.5 | 1.0 ± 0.4 | 1.3 ± 0.1 | 1.4 ± 0.3 | 3.0 ± 1.4 | 8.8 ± 2.2 | 0.5 ± 0.2 |
| 12 | µM | 7.6 ± 0.5 | 1.2 ± 0.7 | 0.8 ± 0.2 | 1.4 ± 0.1 | 21.4 ± 10.1 | 38.3 ± 17.8 | 36.4 ± 11.5 | 52.0 ± 33.4 |
| 13 | µM | 32.2 ± 2.0 | 11.5 ± 1.0 | 11.6 ± 0.5 | 1.0 ± 0.1 | 6.1 ± 1.1 | 8.3 ± 1.3 | 3.2 ± 1.0 | 9.5 ± 0.9 |
| 14 | µM | 26.2 ± 0.9 | 44.5 ± 8.3 | 5.8 ± 0.1 | 31.1 ± 1.6 | 44.5 ± 4.8 | 46.2 ± 9.1 | 41.0 | 22.7 |
| 16 | µM | 38.2 ± 5.1 | 18.1 ± 3.4 | 19.0 ± 5.7 | 15.4 ± 6.0 | 7.8 ± 1.0 | 33.6 ± 2.6 | 58.4 ± 2.5 | 22.1 ± 11.4 |
| 22 | µM | 1.4 ± 0.1 | 1.3 ± 0.6 | 0.5 ± 0.2 | 1.4 ± 0.3 | 2.3 ± 0.3 | 3.7 ± 1.3 | 2.5 ± 0.1 | 2.4 ± 1.1 |
| 24 | µM | 31.7 ± 3.1 | 33.2 ± 7.6 | 18.8 ± 8.0 | 41.8 ± 5.3 | 38.9 ± 4.1 | 49.3 ± 5.0 | 76.3 ± 1.4 | 25.2 ± 0.3 |
| 25 | µM | 33.6 ± 4.5 | 6.4 ± 1.5 | 34.4 ± 0.5 | 34.0 ± 2.9 | 36.4 ± 9.8 | >100 | >100 | 52.0 ± 17.4 |
| 26 | µM | 25.9 ± 0.3 | 8.3 ± 1.1 | 9.9 ± 2.7 | 0.6 ± 0.2 | 6.6 ± 1.3 | 41.1 ± 15.9 | 36.9 ± 0.2 | 21.6 ± 5.4 |
| 27 | µM | 27.7 ± 4.3 | 3.7 ± 1.7 | 4.0 ± 3.7 | 1.9 ± 0.2 | 8.3 ± 2.0 | 38.0 ± 11.8 | 56.5 ± 2.8 | 39.8 ± 10.9 |
| DT | nM | 18.7 ± 4.8 | 4.2 ± 1.8 | 2.2 ± 0.8 | 5.5 ± 1.3 | 4.7 ± 1.2 | 4.3 ± 1.6 | 5.2 ± 1.2 | 3.7 ± 0.7 |
| SP | nM | 1.0 | 6.2 ± 1.8 | 1.5 | 2.2 ± 0.8 | 8.6 ± 1.5 | 9.1 ± 1.6 | 27.9 ± 3.2 | 6.7 ± 4.4 |