Table 3.
Evaluation of 1a–e, 2a–e, 3, and melphalan against normal and malignant cells
| Compound | Normal cells, CC50 (μM)a
|
Tumor cells, CC50 (μM)a
|
||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| HGF | HPC | HPLF | ave | HL-60 | SIb | HSC-2 | SIb | HSC-4 | SIb | |
| 1a | 26 | 31 | 52 | 36 | 12 | 3.0 | 29 | 1.2 | 33 | 1.1 |
| 1b | 6.1 | 6.0 | 9.2 | 7.1 | <3.1 | >2.3 | 5.1 | 1.4 | 6.4 | 1.1 |
| 1c | 19.3 | 30 | 26 | 25 | 1.6 | 16 | 8.2 | 3.1 | 19 | 1.3 |
| 1d | 6.1 | 6.9 | 8.1 | 7.0 | 0.45 | 16 | 3.4 | 2.1 | 7.6 | 0.9 |
| 1e | 6.8 | 5.1 | 9.2 | 7.0 | <3.4 | >2.1 | 5.9 | 1.2 | 6.1 | 1.2 |
| 2a | 4.4 | 5.5 | 5.2 | 5.0 | 0.41 | 12 | 5.2 | 1.0 | 6.5 | 0.8 |
| 2b | 5.8 | 5.4 | 12 | 7.7 | <3.1 | >2.5 | 6.0 | 1.3 | 8.0 | 1.0 |
| 2c | 271 | 227 | 176 | 225 | 35 | 6.4 | 73 | 3.1 | 99 | 2.3 |
| 2d | 4.9 | 5.7 | 9.8 | 6.8 | <3.1 | >2.2 | 6.3 | 1.1 | 5.8 | 1.2 |
| 2e | 4.0 | 5.3 | 4.9 | 4.7 | 0.46 | 10 | 2.5 | 1.9 | 5.2 | 0.9 |
| 3 | 390 | 400 | 400 | 397 | 353 | 1.1 | 165 | 2.4 | 264 | 1.5 |
| Melphalanc | >200 | >200 | >200 | >200 | 6.0 | >33 | 35 | >5.7 | 81 | >2.5 |
a
The CC50 value is the concentration of the compound required to kill 50% of the cells. The figures quoted are the average of two independent determinations which differed by less than 5%. The highest concentrations employed were 400 μM except solubility considerations precluded the use of more than 200 μM of melphalan.
b
The letters SI refer to the selectivity index which was obtained by dividing the average CC50 value for the three normal cells by the CC50 figure of each malignant cell line.
c
The data for melphalan was taken from Ref. 21 copyright (2007) with permission of Elsevier.