Table 5. Carboline analogues from Boehringer-Ingelheim Pharmaceuticals.
| ||||
|---|---|---|---|---|
|
| ||||
| Compd | R1 | R1, R2 | IC50a (nM) | EC50b (nM) |
| 33 | NH2 | 5400 | ||
| 34 |
|
520 | ||
| 35 |
|
820 | ||
| 36 |
|
89 | ||
| 37 |
|
72 | ||
| 38 |
|
34 | ||
| 39 |
|
44 | 1600 | |
| 40 |
|
10 | >5000 | |
| 41 |
|
20 | 1400 | |
| 42 |
|
5 | >5000 | |
| 43 |
|
H, Me | 7 | 8900 |
| 44 |
|
H, Me | 4 | 1670 |
| 45 |
|
H, Me | 3 | 735 |
| 46 |
|
Me, Me | 2 | 430 |
| 47 |
|
-(CH2)3- | 2 | 300 |
Expressed as the inhibition of MK2 in a DELFI assay.
Expressed as the ability to inhibit TNFα production in LPS-stimulated THP-1 cells.
