Table 5.
Substituted Phenyl Ethers as TIQ Reverbα agonists
| |||
|---|---|---|---|
| Compound | R | a Max Inh | EC50 (μM) |
| 6c | H | 0.37 | 0.84 |
| 6f | 4-F | 0.43 | 0.80 |
| 6g | 4-Ph | 0.40 | 0.65 |
| 6h | 4-OMe | 0.38 | 0.12 |
| 6i | 4-OEt | 0.35 | 0.097 |
| 6j | 4-O-n-Pr | 0.45 | 0.077 |
| 6k | 4-O-t-Bu | 0.50 | 0.14 |
| 6l | 4-OCF3 | 0.40 | 0.60 |
| 6m | 4-1,2,4-triazole | 0.35 | 0.12 |
| 6n | 2-OMe | 0.40 | 2.0 |
| 6o | 3-OMe | 0.45 | 0.62 |
| 6p | 3-N(CH3)2 | 0.30 | 0.78 |
| 6q | 3,4-di-OMe | 0.55 | 0.33 |
| 6r | 2,4-diF | 0.45 | 0.71 |
a
results are average of 2 or more experiments. Value = fold change relative to DMSO control at 10 μM compound. The lower the number, the more efficacious the agonist in terms of repressing transcription.