Table 4.
In vitro IDO1/TDO inhibitory activities and cell cytotoxicities of series 4.
| Compound | Structure | IDO a IC50 or % |
TDO a IC50 or % |
H460 a IC50 or % |
MCF7 a IC50 or % |
|---|---|---|---|---|---|
| DX-04-01 |
|
46.2% | 26.5% | 11.96 μM | 8.53μM |
| DX-04-02 |
|
9.7% | 18.0% | 7.69 μM | 35.72 μM |
| DX-04-03 |
|
8.7% | 17.3% | 11.48 μM | 15.44 μM |
| DX-04-04 |
|
11.9% | 23.8% | 5.49 μM | 20.95 μM |
| DX-04-05 |
|
23 μM | 22.4% | 22.89 μM | 42.55 μM |
| DX-04-06 |
|
13.5% | 23.6% | 48.37 μM | 49.34 μM |
| DX-04-07 |
|
38.2% | 21.4% | 27.4 μM | 12.28 μM |
| DX-04-08 |
|
21.2% | 11.2% | 7.5% | 24.9% |
| NLG919 | 0.064 μM | 0.085 μM | NA | NA | |
| Taxol | NA | NA | 6 nM | 15 nM |
a When the calculated IC50 of a compound is >50 μM, we show the inhibition rate (%) at 50 μM. -: no detectable inhibition. NA: not tested.