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Inhibition of the chymotryptic-like activity of purified human 20S proteasome by compounds 1, 6–10. N.D = not determined.
|
R | proteasome IC50 (μM) | NF-κB-Luc EC50 (μM) |
|---|---|---|---|
|
| |||
| 1 | CO2CH2CH3 | 2.5 | 2.5 |
| 6 | CO2H | N.D. | N.D. |
| 7 | CO2CH3 | 5.4 | 7.5 |
| 8 | CO2Bn | 2.4 | 3.5 |
| 9 | CONH2 | >10 | >20 |
| 10 | CO2CH2CH2OH | 3.2 | 10.9 |
