Table 2.
Doubly modified aldehyde derivatives of GC373. GC373 and aldehyde derivatives structures containing modifications at both the P2 and P3 positions are shown, along with SARS-CoV-2 Mpro IC50 and SARS-CoV-2 antiviral EC50 values, both with and without co-administration of efflux inhibitor CP-100356 (+CP). Cytotoxicity assays showed CC50 values of >200 μM for all compounds shown.
| Entry | Structure | IC50 (μM) | EC50 (μM) | EC50 (μM) +CP |
|---|---|---|---|---|
| 1i (PDB 7LCO) |  |
0.14 ± 0.04 | 1.1 ± 0.2 | 0.25 ± 0.1 |
| 1j |  |
0.24 ± 0.09 | 0.8 ± 0.2 | 0.28 ± 0.02 |
| 1k |  |
0.05 ± 0.01 | 0.7 ± 0.1 | 0.27 ± 0.4 |
| 1l |  |
0.43 ± 0.03 | 2.0 ± 0.5 | 1.2 ± 0.8 |