Table 4. Inhibitory Potencies of Selected Indole Derivatives against the ABC Transporters ABCB1, ABCC1, and ABCG2 Obtained in Calcein AM (ABCB1),2,52−59 Daunorubicin (ABCB152,60 and ABCC152,58−60), and Pheophorbide A (ABCG2)2,52−60 Assays Using ABCB1-Expressing A2780/ADR (A), ABCC1-Expressing H69AR (B), and ABCG2-Expressing MDCK II BCRP (C) Cells, Respectivelya.
| no. | ABCB1 calcein AMIC50 ± SEM [μM] | ABCB1 daunorubicinIC50 ± SEM [μM] | ABCC1 daunorubicinIC50 ± SEM [μM] | ABCG2 pheophorbide AIC50 ± SEM [μM] |
|---|---|---|---|---|
| 22 | 24.3 ± 6.4b | n.t. | 17.3 ± 2.2i | 99.5 ± 24.5j |
| 23 | 5.32 ± 1.67b | n.t. | 19.1 ± 3.4i | 43.5 ± 7.5j |
| 24 | 0.983 ± 0.135c | 1.49 ± 0.05f | n.t. | n.t. |
| 30 | 1.51 ± 0.08d | 2.77 ± 0.02g | n.t. | n.t. |
| 31 | 1.40 ± 0.11e | 1.19 ± 0.12h | n.t. | n.t. |
| 34 | 0.960 ± 0.018 | 0.851 ± 0.003 | ||
| 35 | 0.215 ± 0.033 | |||
| 36 | 0.161 ± 0.011 |
Mean ± SEM values of at least three independent experiments are shown.
Constrained to the reference ABCB1 inhibitor 34.
Imax = 66.8 ± 3.3%.
Imax = 61.1 ± 2.1%
Imax = 47.9 ± 4.9%.
Imax = 84.0 ± 2.5%.
Imax = 93.3 ± 2.6%.
Imax = 39.0 ± 2.8%.
Constrained to the reference ABCG2 inhibitor 36; n.t., not tested due to lack of inhibitory activity in the initial screening.