Table 2. Compounds’ IC50 Values and Inhibitory Percentage against SARS-CoV-2 Mpro, as well as Their Cytotoxicity against Vero and THP-1 Cell Linesa.
| CC50 ± SD (μM) |
|||||
|---|---|---|---|---|---|
| compounds | effect at 200 μM (%) | IC50 ± SD (μM) | THP-1 | Vero | obs. |
| 1 | 48.0 | NT | NT | NT | |
| 2 | 68.0 | 4.5 ± 1.8 | 52.9 ± 19.2 | >150 | |
| 1a | 84.0 | ND | NT | NT | SP# |
| 2a | 78.0 | 20.7 ± 8.2 | 78.5 ± 8.1 | >150 | |
| 2b | NA | NT | NT | NT | |
| 2c | 80.4 | 35.8 ± 4.5 | 38.8 ± 4.4 | >150 | |
| 2d | 94.3 | 12.4 ± 2.4 | 28.5 ± 3.2 | >150 | |
| 2e | 99.5 | 2.6 ± 1.0 | 47.0 ± 6.5 | >150 | |
| 2f | 97.0 | 9.5 ± 1.0 | 72.1 ± 7.3 | 48.4 ± 13.2 | |
| 2g | 73.3 | 88.7 ± 11.6 | 32.1 ± 3.4 | 82.1 ± 31.5 | |
| 2h | 45.1 | NT | NT | NT | |
| 2i | 80.0 | 4.0 ± 0.9 | 98.9 ± 5.0 | >150 | |
| 2j | 60.8 | 0.6 ± 1.2 | 22.9 ± 3.2 | >150 | SP# |
| 2k | 41.9 | NT | NT | NT | |
| 2l | 55.5 | 2.8 ± 3.3 | >150 | >150 | SP# |
| 2m | 44.2 | NT | NT | NT | |
| GA | NA | NT | NT | NT | |
| Ebselen (10 μM) | 90 | 3.4 ± 1.0 | NT | NT | |
a
NA: no activity; NT: not tested; ND: not determined; SD: standard deviation; Obs.: observation; SP#: solubility problem observed at the end of the experiment.