Table 3.
In vitro IDO1/TDO inhibitory activities and cell cytotoxicity of series 3.
| Compound | Structure | IDO a IC50 or % |
TDO a IC50 or % |
H460 a IC50 or % |
MCF7 a IC50 or % |
|---|---|---|---|---|---|
| DX-03-01 |
|
26.3% | 10.3% | NA | NA |
| DX-03-02 |
|
24.2% | 13.9% | NA | NA |
| DX-03-03 |
|
19.4% | 11.1% | 5.0% | 22.2% |
| DX-03-04 |
|
11.9% | 20.3% | 12.7% | 34.7% |
| DX-03-05 |
|
31.3% | 12.1% | NA | NA |
| DX-03-06 |
|
25.6% | 12.9% | NA | NA |
| DX-03-07 |
|
33.5% | 15.1% | NA | NA |
| DX-03-08 |
|
15.6% | 11.1% | NA | NA |
| DX-03-09 |
|
5.3% | 6.4% | 40.5% | 37.7% |
| DX-03-10 |
|
13.2% | 21.5% | 7.6% | 24.7% |
| DX-03-11 |
|
2.4 μM | 38.2% | NA | NA |
| DX-03-12 |
|
0.3 μM | 36.4% | 19.3% | 6.6% |
| DX-03-13 |
|
0.5 μM | 38.9% | 13.79 | 21.39 |
| 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.