Table 4.
Cytotoxic activity of the target compounds against MCF-7, HCT-116, HepG-2, MCF-7/ADR cancer cell lines and normal cell lines, HFL-1, WI-38.
| |||||||
|---|---|---|---|---|---|---|---|
| IC50 µMa | |||||||
| Cancerotoxicity |
Normotoxicity |
||||||
| Cpd. | R | MCF-7 | HCT-116 | HepG-2 | MCF-7/ADR | HFL-1 | WI-38 |
| 4a | 4-F | 16.5 ± 0.1 | 6.4 ± 0.1 | 11.3 ± 0.1 | 24.4 ± 1.2 | 45.1 ± 0.2 | 56.7 ± 1.1 |
| 4b | 2-Cl | 11.3 ± 0.1 | 2.5 ± 0.2 | 10.7 ± 0.5 | 13.3 ± 0.5 | 71.9 ± 0.1 | 66.7 ± 0.2 |
| 4c | 3-Cl | 8.5 ± 0.6 | 9.9 ± 0.1 | 11.0 ± 0.2 | 10.9 ± 0.2 | 59.5 ± 1.1 | 61.5 ± 1.2 |
| 4d | 4-Cl | 0.6 ± 0.2 | 1.9 ± 0.4 | 7.2 ± 0.1 | 12.5 ± 0.3 | 77.1 ± 1.1 | 83.0 ± 1.1 |
| 4e | 2-Br | 8.3 ± 0.6 | 5.9 ± 0.4 | 4.9 ± 0.2 | – | 49.5 ± 1.1 | 59.1 ± 1.1 |
| 4f | 3-Br | 69.2 ± 0.3 | 11.5 ± 1.1 | 63.6 ± 3.2 | – | – | – |
| 4g | 4-Br | 5.6 ± 0.1 | 2.2 ± 0.1 | 2.0 ± 0.1 | 19.6 ± 1.0 | 65.3 ± 0.1 | 69.0 ± 1.1 |
| 4h | 4-I | 48.4 ± 0.1 | 27.7 ± 0.3 | 39.2 ± 0.2 | – | – | – |
| 4i | 4-Me | 7.0 ± 0.1 | 2.9 ± 0.1 | 8.8 ± 0.2 | 42.8 ± 2.4 | 71.6 ± 0.3 | 61.7 ± 0.1 |
| 4j | 4-CF3 | 26.8 ± 1.8 | 20.2 ± 1.1 | 5.3 ± 0.1 | – | – | – |
| 4k | 2,4-F2 | 3.0 ± 0.3 | 4.1 ± 0.2 | 8.2 ± 0.6 | 11.5 ± 0.6 | 59.6 ± 0.1 | 47.3 ± 0.2 |
| 4l | 2,6-F2 | 15.4 ± 0.2 | 77.7 ± 0.3 | 28.5 ± 0.4 | – | – | – |
| 4m | 2,3-Cl2 | 9.1 ± 0.2 | 42.0 ± 0.2 | 11.8 ± 0.2 | – | – | – |
| 4n | 2,4-Cl2 | 1.8 ± 0.1 | 1.7 ± 0.2 | 7.3 ± 0.2 | 15.5 ± 0.2 | 71.7 ± 0.1 | 61.9 ± 0.3 |
| 4o | 2,5-Cl2 | 3.8 ± 0.3 | 8.3 ± 0.2 | 46.6 ± 0.1 | – | – | – |
| 4p | 2,6-Cl2 | 41.5 ± 0.1 | 18.9 ± 0.2 | 25.9 ± 0.3 | – | – | – |
| 4q | 3,4-Cl2 | 2.3 ± 0.1 | 1.3 ± 0.1 | 1.5 ± 0.1 | 13.4 ± 0.4 | 75.8 ± 0.2 | 72.8 ± 0.4 |
| 4r | 2,5-Br2 | 4.9 ± 0.5 | 5.3 ± 0.4 | 6.8 ± 0.5 | – | 38.1 ± 0.2 | 33.9 ± 0.4 |
| 4s | 3,5-Br2 | 13.6 ± 0.2 | 15.0 ± 2.6 | 13.4 ± 1.1 | – | – | – |
| 4t | 2-Cl-6-F | 100.0 ± 1.3 | 96.5 ± 2.0 | 48.1 ± 1.3 | – | – | – |
| 4u | 2-F-4-CF3 | 0.2 ± 1.3 | 14.7 ± 2.3 | 10.6 ± 0.9 | 19.7 ± 0.8 | 55.3 ± 0.1 | 60.3 ± 0.1 |
| 4v | 2,4-(OMe)2 | 100.0 ± 0.2 | 49.9 ± 0.5 | 93.2 ± 0.2 | – | – | – |
| 4w | 3,4-(OMe)2 | 2.6 ± 0.5 | 6.2 ± 0.3 | 52.3 ± 0.4 | 11.5 ± 0.6 | 47.1 ± 0.2 | 52.9 ± 0.3 |
| 4x | 2,3,4-(OMe)3 | 96.1 ± 0.6 | 36.6 ± 0.1 | 59.7 ± 0.3 | – | – | – |
| 4y | 3,4,5-(OMe)3 | 26.1 ± 0.1 | 15.4 ± 0.1 | 8.8 ± 0.2 | – | 34.1 ± 0.2 | 29.9 ± 0.4 |
| 4z | 3,5-Br2-2-OMe | 5.8 ± 0.04 | 6.8 ± 0.1 | 3.5 ± 0.2 | – | 33.3 ± 0.1 | 39.6 ± 0.4 |
| A | – | 7.5 ± 0.03 | 3.2 ± 0.1 | 5.7 ± 0.1 | – | – | – |
| B | – | 0.8 ± 0.01 | 0.9 ± 0.02 | 1.7 ± 0.4 | 18.6 ± 0.2 | – | – |
aIC50 values expressed in µM as the mean values of triplicate wells from at least three experiments and are reported as the mean ± standard error, A = Vinblastine and B = Doxorubicin.