Table 1.
Cytotoxicity, CD98 down-regulation and vacuolation profiles of the new C-3-arylalkyl chain variants of analog 3

| Comp. | IC50 (μM) [95% CI] | %CD98 down-regulation | Vacuolation score | |||||
|---|---|---|---|---|---|---|---|---|
| 2.5 μM | 10 μM | 40 μM | 2.5 μM | 10 μM | 40 μM | |||
| 1 | 2.1 | [1.9, 2.4] | 30 | 63 | n.d. | +++ | +++ | n.d. |
| 3 | 2.1 | [2.0, 2.2] | 41 | 66 | n.d. | ++ | +++ | n.d. |
| 4 | 10.9 | [8.7, 13.7] | 11 | 14 | 51 | n.d. | 0 | 0 |
| 5 | 10.2 | [8.7, 12.0] | 5 | 18 | 61 | n.d. | 0 | 0 |
| 6 | 8.4 | [7.0, 10.1] | 5 | 33 | 61 | n.d. | 0 | 0 |
| 7 | 15.1 | [11.2, 20.3] | −15 | −8 | 23 | n.d. | 0 | 0 |