Table 5. Optimization of ring B.
| ||||
Compound | R | R′ | Inhibition @10 μM (%) | PBD |
23 | Cl | H | 33 (IC50 18) | 5OSZ |
CAM4712 | Cl | Cl | 80 (IC50 7) | 5OTY |
31 | Me | H | 30 | 5OYF |
32 | CF3 | H | 23 | 6EHU |
33 | OMe | H | 41 | 5OTQ |
34 | OCF3 | H | 39 | n.a. |
| ||||
Compound | R | R′ | Inhibition @10 μM (%) | PBD |
23 | Cl | H | 33 (IC50 18) | 5OSZ |
CAM4712 | Cl | Cl | 80 (IC50 7) | 5OTY |
31 | Me | H | 30 | 5OYF |
32 | CF3 | H | 23 | 6EHU |
33 | OMe | H | 41 | 5OTQ |
34 | OCF3 | H | 39 | n.a. |