Table 1. ABCG2 Inhibitory Activity in Comparison to Reference Compounds, Chalcones 16a–f, and Ketones 17a–f.
| ABCG2a |
|||
|---|---|---|---|
| compd | IC50 (μM)b | Imax (%)c | clogPd |
| FTC | 0.731 ± 0.092 | 100 | 1.23 |
| Tariquidar | 0.526 ± 0.085 | 69 ± 5 | 6.38 |
| 16a | 4.08 ± 0.29 | 79 ± 4 | 6.51 |
| 16b | 2.13 ± 0.47 | 72 ± 8 | 6.18 |
| 16c | 2.83 ± 0.30 | 81 ± 5 | 5.46 |
| 16d | 0.88 ± 0.02 | 86 ± 10 | 6.97 |
| 16e | 1.55 ± 0.36 | 97 ± 3 | 6.64 |
| 16f | 2.72 ± 0.54 | 111 ± 4 | 5.92 |
| 17a | 6.73 ± 1.02 | 77 ± 1 | 4.45 |
| 17b | 14.39 ± 11.8 | 55 ± 2 | 4.12 |
| 17c | 1.13 ± 0.27 | 47 ± 1 | 3.40 |
| 17d | 8.76 ± 1.59 | 77 ± 1 | 4.91 |
| 17e | 23.24 ± 4.36 | 79 ± 1 | 4.58 |
| 17f | 6.65 ± 1.27 | 86 ± 2 | 3.86 |
a
Hoechst 33342 microplate assay using ABCG2-overexpressing MCF-7/Topo cells.
b
Relative IC50 value23calculated using GraphPad Prism 7 four parameter curve fitting and presented as mean values ± SEM from three independent experiments performed in triplicate.
c
Maximal inhibitory effects (%) are expressed as inhibition caused by the highest concentration (100 μM) of the compound, relative to the inhibitory effect caused by 10 μM FTC (100% inhibition).
d
Calculated values using ACD/Laboratories I-Lab 2.0 ilab.acdlabs, Algorithm Version: v5.0.0.184.