Table 1. Inhibition data of CDK8/CycC for compounds 5a-i, using Staurosporine as a standard inhibitor.
| Comp. | R | R‘ | % enzyme inhibition ± SD(20 µM) | IC50(µM) |
|---|---|---|---|---|
| 5a | 6-Br | SO2NH2 | 83.91 ± 1.83 | 3.98 |
| 5b | 6-OCH3 | SO2NH2 | 63.365 ± 2.31 | 5.34 |
| 5c | 7-Cl-6-F | SO2NH2 | 37.925 ± 1.31 | No inhibition |
| 5d | 6-Br | NHSO2CH3 | 88.59 ± 0.97 | 0.639 |
| 5e | 6-OCH3 | NHSO2CH3 | 85.875 ± 0.94 | 1.42 |
| 5f | 7-Cl-6-F | NHSO2CH3 | 27.225 ± 8.46 | No inhibition |
| 5g | 6-Br | SO2NHCH3 | 22.425 ± 1.02 | No inhibition |
| 5h | 6-OCH3 | SO2NHCH3 | 18.655 ± 0.48 | No inhibition |
| 5i | 7-Cl-6-F | SO2NHCH3 | 31.96 ± 0.82 | No inhibition |
| Staurosporine | 1.00 E–4 | |||