IC50 of the target compounds against SW480, A549, Hek293, MCF7, MCF10A in MTT assay for a 72 h incubation period.
| Entry | Compound | % eea,b | SW480 (μM) | A549 (μM) | Hek293 (μM) | MCF7 (μM) | MDA-MB-231 (μM) | MCF10A (μM) |
|---|---|---|---|---|---|---|---|---|
| 1 | (1a) | — | 32.2 ± 2.9 | 54.7 ± 2.1 | 63.7 ± 4.5 | 1.39 ± 0.2 | 2.95 ± 0.4 | 1.80 ± 0.3 |
| 2 | (1b) | >98 | 8.9 ± 0.8 | 53.8 ± 1.6 | 23.1 ± 1.4 | 1.34 ± 0.2 | 1.79 ± 0.2 | 1.08 ± 0.2 |
| 3 | (1c) | — | 26.6 ± 2.3 | 41.5 ± 2.3 | 26.9 ± 1.7 | 1.50 ± 0.2 | 2.40 ± 0.7 | 1.54 ± 0.2 |
| 4 | (S)-(2a) | 80 | 62.4 ± 4.2 | >100 | >100 | |||
| 5 | (S)-(2b) | 86 | 9.9 ± 1.6 | 28.3 ± 1.5 | 12.4 ± 1.1 | 1.75 ± 0.2 | 3.10 ± 0.4 | 1.33 ± 0.2 |
| 6 | (S)-(2d) | 78 | 28.2 ± 3.1 | 72.1 ± 4.5 | 50.3 ± 2.2 | |||
| 7 | (S)-(2e) | 87 | 36.6 ± 1.1 | 95.9 ± 5.1 | 38.0 ± 2.3 | |||
| 8 | (S)-(2f) | 75 | 29.5 ± 2.8 | >100 | 64.0 ± 4.7 | |||
| 9 | (S)-(2g) | 86 | 31.8 ± 2.3 | >100 | 33.7 ± 1.5 | |||
| 10 | (S)-(2h) | 74 | >100 | >100 | >100 | |||
| 11 | (S)-(2j) | 95 | 18.9 ± 1.7 | 29.3 ± 3.2 | 87.3 ± 6.4 | 2.039 ± 0.3 | 1.622 ± 0.2 | 1.105 ± 0.2 |
| 12 | (2k) | 98 | >100 | >100 | >100 | |||
| 13 | (R)-(2a) | 74 | 75.3 ± 3.5 | >100 | >100 | |||
| 14 | (R)-(2b) | 86 | 8.7 ± 0.5 | 23.5 ± 1.4 | 14.0 ± 1.1 | |||
| 15 | (R)-(2c) | 67 | >100 | >100 | >100 | |||
| 16 | (R)-(2d) | 76 | 32.1 ± 1.6 | 77.3 ± 3.9 | 53.5 ± 2.8 | |||
| 17 | (R)-(2e) | 87 | 75.8 ± 4.3 | >100 | >100 | |||
| 18 | (R)-(2f) | 89 | 62.5 ± 3.7 | 98.0 ± 4.7 | 46.4 ± 2.7 | |||
| 19 | (R)-(2h) | 94 | >100 | >100 | >100 | |||
| 20 | (R)-(2j) | 92 | 28.7 ± 1.8 | 65.9 ± 2.8 | 36.1 ± 1.9 | 1.49 ± 0.3 | 1.41 ± 0.2 | 1.02 ± 0.2 |
| 21 | CDDP c | 12.8 ± 1.2 | 6.0 ± 0.9 | 15.9 ± 2.0 | 14.65 ± 3.89 | 18.7 ± 4.77 | 33.76 ± 2.05 |
a
Determined using HPLC with a chiral column.10
b
This was the assigned configuration to carbon-3 of the oxindole unit.
c
Cisplatin.