Table 1.
Antiproliferative activity of target compounds 15a–d, 16a,b, 17a–d against cancer cells (IC50 values 1, µM); the dose–response curves are presented in Figures S1–S5.
| Cell Line | |||||
|---|---|---|---|---|---|
| Compound | A-431 | T47D | MCF7 | HCC1954 | SKBR3 |
| c-Met Status | ++ | - | - | +++ | - |
| 15a | >25 | 6.1 | 28.1 | 5.7 | >25 |
| 15b | >25 | 14.2 | >25 | 9.1 | >25 |
| 15c | >25 | >25 | >50 | 6.7 | 10.8 |
| 15d | >25 | >25 | >50 | 20.3 | >25 |
| 16a | 12.3 | 8.2 | 19.4 | >25 | >25 |
| 16b | >25 | 3.8 | >25 | >25 | >25 |
| 17a | >25 | >25 | >25 | >25 | >25 |
| 17b | >25 | >25 | >25 | >25 | >25 |
| 17c | >25 | >25 | >25 | >25 | >25 |
| 17d | >25 | >25 | >25 | >25 | >25 |
| 3 | 20.6 | 7.2 | 14.8 | 9.8 | 22.6 |
| c abozantinib | 11.2 | 4.4 | 9.0 | 8.7 | 18.1 |
1 Cells were incubated with compounds for 72 h; data are shown as the averages of three experiments. Standard deviations were within 10% and not demonstrated for the simpler reading of the results. “-”, “++” and “+++” indicates the level of c-Met expression: almost no c-Met, average c-Met expression and high level of c-Met expression, respectively