Table 1.
Inhibition of QR2 and Aromatase by Compound 1 and Its Analogues
| Quinolinones | QR2 IC50 (μM) | Aromatase IC50 (μM) | Cytotoxicity IC50 (μM) |
|||
|---|---|---|---|---|---|---|
| Hepa 1c1c7 | MCF7 | LNCaP | LU | |||
| 1 | 54.1 ± 6.7 | 3.92 ± 0.67 | >85.81 | >85.81 | >85.81 | >85.81 |
| 1a | 10.8 ± 2.1 | >98.49 | >98.49 | >98.49 | >98.49 | >98.49 |
| 1b | 6.2 ± 0.8 | 1.25 ± 0.03 | >92.14 | >92.14 | >92.14 | >92.14 |
| 1c | >500 | >125.7 | >125.7 | >125.7 | >125.7 | >125.7 |
| 1d | 18.2 ± 3.1 | >115.6 | >115.6 | >115.6 | >115.6 | >115.6 |
| 1e | 24.1 ± 3.4 | >105.8 | >105.8 | >105.8 | >105.8 | >105.8 |
| 1f | 5.8 ± 0.9 | 2.02 ± 0.1 | >98.48 | >98.48 | >98.48 | >98.48 |
| 1g | 29.3 ± 3.4 | 31.5 ± 3.1 | >91.29 | >91.29 | >91.29 | >91.29 |
| 1h | 9.3 ± 2.3 | 5.76 ± 0.07 | >85.80 | >85.80 | >85.80 | >85.80 |
| 1i | 8.8 ± 1.1 | >91.29 | >91.29 | >91.29 | >91.29 | >91.29 |
| 1j | 1.9 ± 0.2 | 0.96 ± 0.02 | >85.80 | >85.80 | >85.80 | >85.80 |
| 1k | 10.8 ± 1.5 | 26.8 ± 13.77 | >91.22 | >91.22 | >91.22 | >91.22 |
| 1l | 4.1 ± 0.6 | 0.96 ± 0.01 | >85.74 | >85.74 | >85.74 | >85.74 |
| 1m | 10.0 ± 1.4 | 18.47 ± 3.7 | >80.29 | >80.29 | >80.29 | >80.29 |
| 1n | 7.0 ± 1.1 | 2.72 ± 0.02 | >76.01 | >76.01 | >76.01 | >76.01 |
| 1o | 6.0 ± 0.6 | 14.8 ± 0.65 | 34.52 | 42.95 | 45.76 | 35.28 |
| 1p | 10.8 ± 1.3 | 0.10 ± 0.01 | 70.73 | >76.01 | >76.01 | 68.47 |
| 1q | >500 | 5.68 ± 0.24 | >71.66 | >71.66 | >71.66 | >71.66 |
| 1r | >500 | 0.76 ± 0.02 | >68.23 | >68.23 | >68.23 | >68.23 |
| 11 | >500 | >90.4 | NTa | NT | NT | NT |
| 12 | >500 | >98.4 | 54.14 | 60.53 | 58.07 | 49.22 |
| Resveratrol6 | 0.96 +/− 0.13 | NT | NT | NT | NT | NT |
| Melatonin6 | 11.3 +/− 2.1 | NT | N | NT | NT | NT |
| Aminoglutethimide | 0.27 | NT | NT | NT | NT | |
a
Not tested.