Table 2.
Inhibition of canonical NF-κB signalling by simplified helenalin analogues. Values are the mean ± S.D. from n ≥ 3 biological replicates and were normalized to a no compound, induced control.
| no Michael acceptors |
NF-κB activity (%; Mean ± S.D.) | ||
|---|---|---|---|
|
| |||
| 250 µM | 100 µM | ||
| 9 | 86 ± 1 | 91 ± 3 | |
| 10 | 86 ± 5 | 97 ± 8 | |
| 13 | 78 ± 5 | 84 ± 1 | |
| 15 | 99 ± 8 | 99 ± 7 | |
| 16 | 79 ± 6 | 82 ± 2 | |
|
| |||
| enone only | 250 µM | 100 µM | 50 µM |
|
| |||
| 11 | 50 ± 5 | 85 ± 3 | 92 ± 6 |
| 12 | 34 ± 4 | 69 ± 4 | 93 ± 11 |
| 14 | 43 ± 4 | 73 ± 3 | - |
| 17 | 78 ± 9 | 86 ± 12 | 95 ± 5 |
| 18 | 63 ± 4 | 83 ± 8 | 88 ± 6 |
| S4 | 23 ± 4 | 62 ± 2 | - |
|
| |||
| butyrolactone only | 50 µM | 20 µM | 10 µM |
| 19 | 11 ± 2 | 43 ± 1 | 71 ± 2 |
| 20 | 12 ± 1 | 42 ± 2 | 69 ± 2 |
| 1b[a] | 7 ± 1 | 16 ± 8 | 52 ± 17 |