Table 2.
Compound 7d effectively sensitizes drug selective ABCG2-overexpressing cancer cells to the substrate anticancer drugs
| Drugs | IC50 ± SDa (nM) (Resistance fold)
|
|
|---|---|---|
| H460 | H460/MX20 | |
| Mitoxantrone | 108.5 ± 18.9 (1.0) b | 9353.2 ± 876.8 (86.2) |
| +compound 7d 2.5 μM | 98.5 ± 9.5 (0.9) | 2390.0 ± 517.3 (22.0)* |
| +compound 7d 5 μM | 74.9 ± 16.0 (0.7) | 2253.3 ± 432.1 (20.8)* |
| +compound 7d 10 μM | 87.5 ± 6.6 (0.8) | 680.9 ± 256.1 (6.3)* |
| +FTC 2.5 μM | 86.8 ± 8.7 (0.8) | 525.4 ± 120.4 (4.8)* |
| SN-38 | 52.4 ± 5.6 (1.0) b | 9702.8 ± 1008.4 (185.2) |
| +compound 7d 2.5 μM | 55.4 ± 7.3 (1.1) | 914.6 ± 83.9 (17.5)* |
| +compound 7d 5 μM | 41.2 ± 13.2 (0.8) | 426.5 ± 52.6 (8.1)* |
| +compound 7d 10 μM | 46.2 ± 8.7(0.9) | 281.7 ± 49.3 (5.4)* |
| +FTC 2.5 μM | 40.6 ± 9.4(0.8) | 264.1 ± 28.0 (5.0)* |
| Cisplatin | 9608.9 ± 733.1 (1.0) b | 10356.6 ± 1065.2 (1.1) |
| +compound 7d 2.5 μM | 8917.6 ± 681.7 (0.9) | 9339.4 ± 729.4 (1.0) |
| +compound 7d 5 μM | 10323.4 ± 1087.8 (1.1) | 9162.6 ± 821.6 (1.0) |
| +compound 7d 10 μM | 8172.9 ± 765.5 (0.9) | 8251.4 ± 743.5 (0.9) |
| +FTC 2.5 μM | 11568.4 ± 980.1 (1.2) | 10767.2 ± 850.4 (1.1) |
a
Values represent mean ± SD of at least three independent experiments, each performed in triplicate.
b
Resistance fold was calculated by dividing the IC50 values of mitoxantrone, SN-38, or cisplatin of H460/MX20 cells in the absence or presence of reversal agents by the IC50 values of substrates of H460 cell line.
*
: p<0.05