Table 1.
The results for the Tdp1 activity inhibition at 50% (IC50) values of the derivatives. Additionally, the CC50 (50% cytotoxic concentration) values are given for cervical cancer (HeLa) and colorectal (HCT-116, SW837) human cancer cell lines.
| Structure | IC50, μM | CC50, μM HeLa | CC50, μM HCT-116 | CC50, μM SW837 | |
|---|---|---|---|---|---|
1,2,4-Triazole derivatives
| |||||
| 20a |
|
0.54 ± 0.09 | 85 ± 23 | 27 ± 6 | 52 ± 6 |
| 20b |
|
1.5 ± 0.3 | >100 | >100 | 41 ± 4 |
| 20c |
|
5.3 ± 1.7 | 64 ± 6 | 16 ± 7 | 41 ± 6 |
| 20d |
|
5.6 ± 0.6 | 31± 11 | 20 ± 9 | 17 ± 5 |
| 20e |
|
6.2 ± 2.2 | 24 ± 16 | 15 ± 5 | 40 ± 4 |
| 20f |
|
7.5 ± 1.8 | 15 ± 2 | 54 ± 5 | 46 ± 6 |
| 20g |
|
0.57 ± 0.14 | 74 ± 17 | 34 ± 6 | 40 ± 4 |
1,3,4-Thiadiazole derivatives
| |||||
| 25a |
|
0.35 ± 0.05 | >100 | >100 | >100 |
| 25b |
|
2.59 ± 0.48 | >100 | 66 ± 6 | 83 ± 8 |
| 25c |
|
0.45 ± 0.09 | >100 | >100 | >100 |