Table 2.
The inhibitory activity (IC50 uM) of compounds (7 (a, b), 9–42) and selectivity-fold against HCT-116, SD never exceeded 5%, (n = 9), and treatment for 48 h
| Compound | IC50 uM | Selectivity Fold | Compound | IC50 uM | Selectivity Fold | ||
|---|---|---|---|---|---|---|---|
| HCT-116 | CaCo-2 | HCT-116 | CaCo-2 | ||||
| 7a | 74.98 | 913.8 | 12 | 26 | 139.3 | 469.3 | 3.4 |
| 7b | 101.0 | 178.7 | 1.8 | 27 | 332.2 | 479.0 | 1.4 |
| 9 | 60.39 | 95.3 | 1.6 | 28 | 119.7 | 205.1 | 1.7 |
| 10 | 23.41 | 58.08 | 2.5 | 29 | 11.9 | 76.0 | 6 |
| 11 | 30.82 | 69.94 | 2.3 | 30 | 15.6 | 47.5 | 3 |
| 12 | 83.22 | 128.77 | 1.6 | 31 | 51.6 | 59.8 | 1 |
| 13 | 27.14 | 77.18 | 2.8 | 32 | 170.6 | NOT ACTIVE | - |
| 14 | 56.99 | 116.7 | 2.0 | 33 | 38.7 | 67.3 | 1.7 |
| 15 | 101.1 | 171.0 | 1.7 | 34 | 121.5 | 200 | |
| 16 | 28.43 | 70.52 | 2.5 | 35 | 37.8 | 32.9 | 0.9 |
| 17 | 127.5 | 194.4 | 1.5 | 36 | 76.86 | 504 | 6.6 |
| 18 | 207.7 | 652.4 | 3.0 | 37 | 447.1 | 756 | 1.7 |
| 19 | 39.08 | 94.12 | 2.4 | 38 | 476.7 | NOT ACTIVE | - |
| 20 | 22.95 | 84.01 | 3.7 | 39 | 2304 | NOT ACTIVE | - |
| 21 | 43.68 | 235.77 | 5.4 | 40 | 65.4 | 61.9 | 0.9 |
| 22 | 37.42 | 98.26 | 2.6 | 41 | 167.1 | 325.6 | 1.9 |
| 23 | 39.11 | 60.57 | 1.5 | 42 | 181 | 346 | 1.9 |
| 24 | 51.39 | 199.26 | 3.9 | LY294002 | 7.4 | ||
| 25 | 229.8 | 385.7 | 1.7 | ||||