Table 2.
Enzyme inhibition data for 8TQ and 8TQ derivatives. Data listed includes inhibitory values against off-target metalloenzymes and cytotoxicity against the HCT 116 cell line. All IC50 values listed are in μM. Reported IC50 values represents the average value obtained from at least three independent measurements, with the standard deviation reported as the error.
| Cmpd | Structure | Rpn11 | Csn5 | HDAC1 | HDAC6 | MMP2 | 5-LO | hCAII | HCT 116 Cytotoxicity |
|---|---|---|---|---|---|---|---|---|---|
| 8TQ | H | 2.8±0.4 | 10.3±2.3 | >200 | >200 | >200 | >200 | >200 | 1.6±0.7 |
| 9c | 2-Me | >100 | >100 | N.D | N.D | >200 | N.D | N.D | >50 |
| 10c | 3-Me | 1.6±0.6 | 7.1±1.6 | >50 | >200 | >200 | >200 | >40 | 2.6±0.5 |
| 11c | 4-Me | 5.7±2.0 | 25.1±6.1 | >200 | >200 | >200 | >200 | >200 | >10 |
| 12c | 5-Me | 2.5±1.3 | 2.9±1.1 | >200 | >200 | >200 | >200 | >200 | 3.4±1.1 |
| 13c | 6-Me | 0.9±0.3 | 1.6±0.6 | >50 | >50 | >200 | >200 | >100 | 2.1±1.2 |