Table 1. STS Inhibitory Effect of Compounds 4a–m and Reference Inhibitors 5g and 5l Using the Radioisotope Enzymatic Assay at a 0.5 μM Inhibitor Concentration.
| no. | R | residual STS activity [%]a |
|---|---|---|
| 4a | 3-Cl | 19.49 ± 0.97 |
| 4b | 3,5-diCl | 13.32 ± 0.67 |
| 4c | 3-Br | 24.05 ± 1.20 |
| 4d | 3-I | 13.23 ± 0.66 |
| 4e | 3-CH3 | 34.23 ± 1.71 |
| 4f | 3,5-diCH3 | 52.45 ± 2.62 |
| 4g | 3-OCH3 | 43.35 ± 2.17 |
| 4h | 3,5-diOCH3 | 55.11 ± 2.76 |
| 4i | 3-CH2CH3 | 14.51 ± 0.73 |
| 4j | 3-CH(CH3)2 | 18.10 ± 0.90 |
| 4k | 3-NO2 | 28.88 ± 1.44 |
| 4l | 3,5-diBr | 28.88 ± 1.44 |
| 4m | 3,5-diI | 11.78 ± 0.59 |
| 5g | 3-F | 37.92 ± 1.90 |
| 5l | 3,5-diF | 17.34 ± 0.87 |
a
Substrate: [3H]E1S, 3 nM; experiments were carried out in triplicate.