Table 6.
TLR signaling inhibition by C3 BSC pyrazoles with electron-donating groups.
 | ||||||
|---|---|---|---|---|---|---|
| Cmpd | R | IC50 (μM) | ||||
| TLR9 | TLR7 | TLR2 | TLR4 | Tox. | ||
| 61 | 3,4-(OMe)2 | 8.26 ± 0.34 | 4.68 ± 1.16 | > 50 | > 50 | 40.9 ± 6.4 |
| 62 | 3,4,5-(OMe)3 | 5.45 ± 0.80 | 2.25 ± 0.27 | 2.49 ± 0.06 | 1.13 ± 0.39 | 16.90 ± 0.01 |
| 63 | 2,4,5-(OMe)3 | 7.62 ± 0.41 | 5.97 ± 1.33 | > 50 | 27.3 ± 2.8 | 22.8 ± 7.0 |
| 64 | 3,4,6-(OMe)3 | 8.40 ± 0.01 | > 50 | > 50 | > 50 | 26.5 ± 4.3 |
| 65 | 2,3,4-(OMe)3 | 10.8 ± 0.1 | > 50 | > 50 | > 50 | > 50 |
| 66 | 3,5-(OMe)2-4-OEt | 9.68 ± 0.82 | > 50 | > 50 | > 50 | > 50 |
| 67 | 3,4,5-(OEt)3 | 11.0 ± 1.1 | 1.48 ± 0.02 | > 50 | > 50 | 20.0 ± 0.2 |
| 68 | 3-OMe-4-OEt | 12.8 ± 0.3 | > 50 | > 50 | > 50 | > 50 |
| 69 | 5-OMe-3,4-dioxymethylene | 7.03 ± 0.29 | 0.79 ± 0.09 | > 50 | > 50 | > 50 |
| 70 | 3,5-(Me)2-4-OMe | 7.04 ± 0.24 | 2.25 ± 0.17 | 15.3 ± 0.3 | 17.3 ± 0.5 | 13.9 ± 0.9 |
| 71 | 3-Cl-4-OMe | 7.78 ± 0.34 | > 50 | > 50 | > 50 | 19.9 ± 1.4 |