Table 2. The 17β-HSD10 inhibition rate and toxicity of compounds 10–16.
| |||
|---|---|---|---|
| Compounds | R2 | IRa (%) at 5 μM | HepaRG MTT IC50b (μM) |
| 8 |
|
42.20 ± 4.31 | 3.63 ± 1.01 |
| 9 |
|
57.17 ± 4.19 | 5.06 ± 1.25 |
| 10 |
|
64.97 ± 5.01 | 6.28 ± 0.68 |
| 11 |
|
54.25 ± 4.61 | 22.15 ± 2.35 |
| 12 |
|
77.01 ± 6.41 | 19.66 ± 3.21 |
| 13 |
|
66.17 ± 6.48 | 8.90 ± 1.25 |
| 14 |
|
62.03 ± 5.01 | 11.45 ± 2.15 |
| 15 |
|
78.95 ± 4.40 | 1.91 ± 0.98 |
| 16 |
|
75.90 ± 5.64 | 5.91 ± 2.15 |
| 17β-HSD10-IN-1 | 88.25 ± 6.34 | 75.52 ± 4.36 | |
a
The inhibition rate of compounds against 17β-HSD10 at 5 μM was determined.
b
Detecting the cytotoxicity of compounds using HepaRG cells. All experimental results were repeated three times, and the values were displayed as means ± SD.