Table 4.
In vitro cytotoxicity of 10f, 10h, 10k and 10n in P-gp overexpressed cell lines.
| Compound | IC50 ± SD (μM) | RIa | IC50 ± SD (μM) | RI | ||
|---|---|---|---|---|---|---|
|
|
|
|||||
| KB-3-1 | KB-C2 | SW620 | SW620/Ad300 | |||
| 10f | 1.36 ± 0.19 | 0.17 ± 0.09 | 0.13 | 0.16 ± 0.04 | 0.027 ± 0.006 | 0.17 |
|
| ||||||
| 10h | 1.39 ± 0.41 | 0.18 ± 0.05 | 0.13 | 0.19 ± 0.09 | 0.06 ± 0.02 | 0.32 |
|
| ||||||
| 10k | 1.71 ± 0.22 | 0.25 ± 0.05 | 0.15 | 0.24 ± 0.09 | 0.05 ± 0.03 | 0.21 |
|
| ||||||
| 10n | 1.28 ± 0.25 | 0.44 ± 0.28 | 0.34 | 0.31 ± 0.05 | 0.10 ± 0.04 | 0.32 |
|
| ||||||
| MX-106 | 1.25 ± 0.10 | 0.33 ± 0.12 | 0.26 | 0.15 ± 0.01 | 0.03± 0.01 | 0.20 |
|
| ||||||
| YM-155 | 0.0049 ± 0.0005 | 37.30 ± 3.97 | 7612.24 | 0.0039 ± 0.0056 | 23.37 ± 2.37 | 5992.31 |
|
| ||||||
| Paclitaxel | 0.0005 ± 0.0001 | 0.25 ± 0.01 | 500.00 | 0.030 ± 0.001 | 1.97 ± 0.36 | 65.67 |
|
| ||||||
| Doxorubicin | 0.37 ± 0.07 | 1.69 ± 0.44 | 4.57 | 0.21 ± 0.03 | 15.24 ± 2.89 | 72.57 |
|
| ||||||
| Cisplatin | 1.15 ± 0.13 | 1.73 ± 0.11 | 1.50 | 1.79 ± 0.06 | 5.12 ± 0.65 | 2.86 |
a
Resistance index (RI) is calculated by dividing IC50 values on multidrug-resistant cell line M14/MDR1 by IC50 values on the matching sensitive parental cell line M14.