Table 1.
The biological activities of compounds 1-7.a
| Compound | KIX-KID inhibition (μM)b | CREB inhibition (μM)c |
|---|---|---|
| 1 | 2.90 ± 0.81 | 2.29 ± 0.31 |
| 2 | >50 | 30.84 ± 8.40 |
| 3 | >50 | >50 |
| 4 | >50 | 24.45 ± 16.80 |
| 5 | 8.74 ± 1.68 | 4.75 ± 3.88 |
| 6 | 5.19 ± 2.20 | >50 |
| 7 | 9.46 ± 4.15 | 18.96 ± 6.09 |
a
All the biological activities are presented as IC50 with mean ± SD of at least two independent experiments or > 50 if IC50 was not reached at the highest tested concentration, which is 50 μM.
b
KIX-KID inhibition was evaluated by an in vitro renilla luciferase complementation assay.
c
CREB inhibition refers to inhibition of CREB-mediated gene transcription in HEK 293T cells using a CREB reporter assay.