Table 1. In vitro activity (IC50 and Ki values) of DXR inhibitors against TgDXR enzyme.
Compound | IC50 ± S.D. (µM) | Ki (µM) |
---|---|---|
1 | 1.03 ± 0.21 | 0.31a |
2 | 1.23 ± 0.12 | 0.37 |
3 | 0.64 ± 0.38 | 0.19 |
4 | 0.62 ± 0.12 | 0.19 |
5 | 2.45 ± 0.54 | 0.74 |
6 | 3.90 ± 1.06 | 1.18 |
7 | 5.82 ± 1.52 | 2.69 |
8 | 52.14 ± 0.34 | 11.00 |
9 | 2.44 ± 0.43 | 0.74 |
10 | 7.68 ± 0.87 | 2.51 |
The Ki value reported in previous studies is 0.09 µM [37]. Values shown in the table represent the means of three independent experiments each done in duplicate (n = 6) ± S.D.