Table 1.
Evaluation of series 1–3 against human CEM and Molt 4/C8 T-lymphocytes and murine L1210 leukemic cells
| Compound | IC50 (μM)a
|
SIb | IC50 (μM)a | |
|---|---|---|---|---|
| CEM | Molt 4/C8 | L1210 | ||
| 1a | 65.6 ± 33.8 | 146 ± 91 | 2.2 | 52.2 ± 15.8 |
| 1b | 32.6 ± 7.0 | 30.2 ± 19.0 | 1.1 | 26.5 ± 21.7 |
| 1c | 7.91 ± 0.53 | 8.95 ± 0.20 | 1.1 | 8.61 ± 1.85 |
| 1d | 11.4 ± 1.9 | 35.5 ± 7.4 | 3.1 | 11.1 ± 0.9 |
| 1e | 10.6 ± 8.5 | 21.3 ± 14.0 | 2.0 | 5.08 ± 4.52 |
| 2a | 1.42 ± 0.07 | 5.84 ± 1.89 | 4.1 | 1.65 ± 0.10 |
| 2b | 33.1 ± 19.5 | 30.9 ± 18.6 | 1.1 | 22.0 ± 18.5 |
| 2c | 12.2 ± 0.0 | 36.8 ± 2.6 | 3.0 | 42.6 ± 1.7 |
| 2d | 8.22 ± 2.28 | 21.0 ± 13.0 | 2.6 | 6.55 ± 4.29 |
| 2e | 1.15 ± 0.03 | 4.90 ± 2.19 | 4.3 | 1.57 ± 0.05 |
| 3 | >500 | >500 | ~1.0 | >500 |
| Melphalanc | 2.47 ± 0.03 | 3.24 ± 0.79 | 1.3 | 2.13 ± 0.03 |
a
The IC50 value is the concentration of compound required to inhibit the growth of the cells by 50%.
b
The letters SI refer to the selectivity index of each compound which is the ratio of the highest to lowest IC50 values of each compound toward the two T-lymphocytes.
c
The data for melphalan is taken from Ref. 23 copyright (2006) with permission of Elsevier.