Table 1.
In vitro IDO1/TDO inhibitory activities and cell cytotoxicities of series 1.
| Compound | Structure | IDOa IC50 or % |
TDO a IC50 or % |
H460 a IC50 or % |
MCF7 a IC50 or % |
|---|---|---|---|---|---|
| DX-01-01 |
|
9.7% | 8.9% | NA | NA |
| DX-01-02 |
|
2.4% | 10.0% | 39.2% | 43.1 µM |
| DX-01-03 |
|
10.3% | 10.1% | 26.3% | 37.6% |
| DX-01-04 |
|
3.3% | 6.0% | 15.1% | 24.3% |
| DX-01-05 |
|
10.2% | 10.5% | 5.9% | 29.7% |
| DX-01-06 |
|
6.2% | 8.4% | 11.2% | 25.7% |
| DX-01-07 |
|
7.4% | 16.9% | 22.2% | 34.6% |
| DX-01-08 |
|
10.9% | 3.2% | NA | NA |
| DX-01-09 |
|
2.6% | 7.8% | NA | NA |
| DX-01-10 |
|
2.1% | 8.9% | NA | NA |
| DX-01-11 |
|
- | 3.8% | NA | NA |
| DX-01-12 |
|
47.1% | 33.9% | NA | NA |
| DX-01-13 |
|
19.7% | 8.1% | 23.1% | 10.1% |
| DX-01-14 |
|
11.1 μM | 38.2% | NA | NA |
| DX-01-15 |
|
21.3 μM | 35.4% | NA | NA |
| DX-01-16 |
|
23.2 μM | 19.7% | 44.5% | 20.9% |
| DX-01-17 |
|
17.7 μM | 42.2% | NA | NA |
| DX-01-18 |
|
5.4% | - | NA | NA |
| DX-01-19 |
|
- | 7.8% | NA | NA |
| DX-01-20 |
|
15.7% | 3.8% | NA | NA |
| DX-01-21 |
|
9.7% | 9.2% | NA | NA |
| DX-01-22 |
|
13.2% | 4.5% | NA | NA |
| 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.