HNE inhibitory activity in an enzymatic assay, antiradical effects in a cell-based assay of ROS production, and cytotoxicity of new Se-derivatives 3a–d, 4a–p, 6 and 8.
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|---|---|---|---|---|
| Comp. | R | HNE inhibition | Antiradical activity | Cyto-toxicity |
| IC50a (μM) | ||||
| 3b | COOCH2CH3 | N.A.b | 1.8 ± 0.2 | N.A.b |
| 3c | CONH–cC3H5 | N.A.b | 9.7 ± 1.4 | 8.0 ± 1.9 |
| 3d | CONH-3-CH3-Ph | N.A.b | N.A.b | N.A.b |
| 4a | CH3 | 7.7 ± 2.3 | 0.42 ± 0.06 | 10.8 ± 2.4 |
| 4b | C2H5 | 2.6 ± 0.2 | 0.18 ± 0.05 | 8.5 ± 1.8 |
| 4c | CH2CH2CH3 | 2.4 ± 0.4 | 0.33 ± 0.08 | 4.9 ± 0.6 |
| 4d | iC3H7 | 1.2 ± 0.1 | 0.60 ± 0.2 | 9.6 ± 2.2 |
| 4e | C(CH3)3 | 1.8 ± 0.1 | 2.6 ± 0.4 | 13.6 ± 3.1 |
| 4f | nC4H9 | 0.9 ± 0.2 | 0.70 ± 0.2 | 4.2 ± 0.9 |
| 4g | nC5H11 | 3.0 ± 0.4 | N.A.b | N.A.b |
| 4h | OC2H5 | N.A.b | 2.5 ± 0.4 | 15.2 ± 3.2 |
| 4i | CH2COOCH2CH3 | N.A.b | 1.0 ± 0.3 | 8.1 ± 1.7 |
| 4j | cC3H5 | 1.4 ± 0.1 | 0.05 ± 0.01 | 10.4 ± 2.4 |
| 4k | cC5H9 | 2.8 ± 0.2 | 1.4 ± 0.2 | 11.8 ± 2.8 |
| 4l | cC6H11 | 24.1 ± 4.8 | 1.1 ± 0.1 | 12.4 ± 3.4 |
| 4m | Ph | 2.3 ± 0.4 | N.T.c | N.T.c |
| 4n | 3-CH3-Ph | 10.9 ± 2.1 | 7.0 ± 1.3 | N.A.b |
| 4o | 4-OCH3-Ph | 8.7 ± 1.2 | N.T.c | N.T.c |
| 4p | 3-Thienyl | N.A.b | 14.3 ± 2.7 | N.A.b |
| 8 | NH–cC3H5 | N.A.b | 0.90 ± 0.3 | 5.9 ± 1.6 |
| 6 | — | 2.7 ± 0.5 | 6.4 ± 0.4 | N.A.b |
| Ebselen (3a) | H | N.A.b | 0.15 ± 0.02 | 9.5 ± 2.5 |
| Sivelestat | — | 0.044 | — | N.A.b |
IC50 values are presented as the mean ± SD of three independent experiments.
N.A.: no inhibitory activity was found at the highest concentration of compound tested (50 μM) or no cytotoxicity activity was found at the highest concentration of compound tested (25 μM).
N.T.: not tested.