Table 4.
Inhibition of the cell proliferation of U251/U251 EphA2 cells.
| Comp | U251 EphA2 overexpressed*(μM) |
U251 Wild type*(μM) |
Selectivity index wild/overexpressed** |
|---|---|---|---|
| Lead | 2.1 ± 1.05 | 5.2 ± 2.56 | 2.5 ± 2.44 |
| 3a | 6.75 ± 2.40 | 12.62 ± 6.62 | 1.9 ± 1.18 |
| 3b | 7.47 ± 3.98 | 8.07 ± 4.37 | 1.1 ± 0.82 |
| 3c | 51.86 ± 26.07 | 160 ± 80.62 | 3.1 ± 2.20 |
| 3d | 1.60 ± 0.40 | 3.05 ± 0.82 | 1.9 ± 0.70 |
| 3e | 2.45 ± 1.11 | 9.22 ± 5.56 | 3.8 ± 2.84 |
| 3f | 3.18 ± 1.44 | 7.48 ± 4.03 | 2.4 ± 1.66 |
| 5a | 12.70 ± 8.72 | 12.23 ± 8.35 | 1.0 ± .93 |
| 5b | 27.41 ± 15.05 | 24.80 ± 16.01 | 0.9 ± .77 |
| 5c | 7.41 ± 2.98 | 8.34 ± 4.42 | 1.1 ± .75 |
| 5d | 12.06 ± 5.98 | 14.73 ± 9.20 | 1.2 ± .97 |
| 5e | 26.43 ± 11.80 | 53.01 ± 29.78 | 2.0 ± 1.44 |
| 5f | 4.41 ± 2.36 | 10.77 ± 7.23 | 2.4 ± 2.10 |
| 6a | 11.14 ± 7.26 | 8.98 ± 4.61 | 0.8 ± 0.67 |
| 6b | 16.50 ± 9.16 | 8.84 ± 4.36 | 0.5 ± 0.40 |
| 6c | 14.60 ± 8.67 | 35.29 ± 21.98 | 2.4 ± 2.10 |
| 6d | 5.15 ± 3.01 | 17.91 ± 12.66 | 3.5 ± 3.19 |
| 6e | 3.00 ±1.26 | 16.49 ± 10.56 | 5.5 ± 4.21 |
| 6f | 2.70 ± 0.55 | 47.94 ± 21.13 | 17.8 ± 8.62 |
| 7ab | 27.99 ± 14.87 | 45.72 ± 34.86 | 1.6 ± 1.52 |
| 7ac | 30.44 ± 12.63 | 174.01 ± 129.21 | 5.7 ± 4.86 |
| 7ba | 41.41 ± 25.89 | 47.86 ± 26.93 | 1.2 ± 0.97 |
| 7bb | 122.30 ± 59.31 | 128.10 ± 53.59 | 1.0 ± 0.67 |
| 7bc | 9.92 ±6.20 | 8.11 ± 4.42 | 0.8 ± 0.68 |
| 7bd | 4.99 ± 2.32 | 10.12 ± 6.11 | 2.0 ± 1.55 |
| 7bg | 1.90 ± 0.55 | 7.91 ± 2.28 | 4.2 ± 1.70 |
| 7ec | 3.41 ± 1.50 | 2.59 ± 1.24 | 0.8 ± 0.49 |
| 7fc | 5.66 ± 2.94 | 11.69 ± 7.36 | 2.1 ± 1.69 |
The area shaded in gray represent the monomer compounds.
*
IC50 values are reported in μM. included Mean±SD.(n=4)
**
Selectivity index is calculated by taking the wild type average/Overexpressed average included is the error of propagation