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. 2024 Mar 19;15(4):1247–1257. doi: 10.1039/d3md00736g

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
a

IC50 values are presented as the mean ± SD of three independent experiments.

b

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).

c

N.T.: not tested.