Table 2.
Evaluation of 3a–d, g, 4a, c, e, g, i and 5 against some human tumor cell lines.a
Compound | All cell lines, IC50 (μM)c | Colon cancer cells, IC50 (μM)b
|
Leukemic cells, IC50 (μM)b
|
|||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|
COLO 205 | HCC-2998 | HCT-15 | KM12 | SW-620 | Ave | HL-60 (TB) | K-562 | RPMI-8226 | SR | Ave | ||
3aa | 0.31 | 0.36 | 0.19 | 0.30 | 0.04 | 0.07 | 0.19 | 0.20 | 0.20 | 0.03 | 0.02 | 0.11 |
3b | 0.58 | 0.63 | 0.62 | 0.16 | 0.30 | 0.32 | 0.41 | 1.12 | 0.28 | 0.12 | 0.16 | 0.42 |
3c | 0.22 | 0.16 | 0.31 | 0.14 | 0.21 | 0.18 | 0.20 | 0.19 | 0.13 | 0.05 | 0.02 | 0.10 |
3d | 8.51 | 12.3 | 16.6 | 5.89 | 11.2 | 3.80 | 9.96 | 13.2 | 5.89 | 1.17 | 1.78 | 5.51 |
3g | 0.06 | 0.07 | 0.10 | 0.07 | 0.06 | 0.03 | 0.07 | 0.07 | 0.03 | 0.02 | 0.02 | 0.04 |
4aa | 0.24 | 0.16 | 0.17 | 0.17 | 0.13 | 0.05 | 0.14 | 0.29 | 0.05 | 0.13 | 0.03 | 0.13 |
4c | 0.09 | 0.08 | 0.13 | 0.06 | 0.16 | 0.03 | 0.09 | 0.11 | 0.03 | 0.02 | 0.01 | 0.04 |
4e | 0.19 | 0.17 | 0.30 | 0.08 | 0.17 | 0.15 | 0.17 | 0.23 | 0.10 | 0.03 | 0.05 | 0.10 |
4g | 0.05 | 0.06 | 0.10 | 0.03 | 0.04 | 0.05 | 0.06 | 0.04 | 0.03 | 0.05 | 0.01 | 0.03 |
4i | 1.66 | 1.66 | 1.74 | 1.17 | 0.69 | 0.76 | 1.20 | 1.74 | 0.53 | 0.35 | 0.46 | 0.77 |
5 | 0.19 | 0.19 | 0.18 | 0.20 | 0.16 | 0.06 | 0.16 | 0.25 | 0.04 | 0.04 | 0.04 | 0.09 |
5-Fluorouracil | 29.5 | 3.39 | 5.75 | 6.61 | 7.94 | 18.6 | 8.46 | 85.1 | 126 | 3.55 | 60.3 | 68.7 |
Melphalan | 19.1 | 32.4 | 52.5 | 36.3 | 57.5 | 26.9 | 41.1 | 0.38 | 195 | 28.2 | 3.24 | 56.7 |
The data for 3a and 4a have been published previously [9].
The IC50 values are the concentrations of the compounds which inhibit tumor cell growth by 50%.
As indicated in the experimental section, the IC50 values of 3d and 5-fluorouracil towards a few cell lines were not generated due to their being somewhat refractory to the compounds.