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. 2022 Jun 7;204:105350. doi: 10.1016/j.antiviral.2022.105350

Table 3.

Biological profile of synthesized derivatives of hit 7

Compound Structure Antiviral Activity EC50a (μM) Cytotoxicity CC50b (μM) SIc Mpro Inhibitory Activity IC50d (μM)
7 Image 33 >50 >500 >10 110.7 ± 2.2
31 Image 34 >50 >250 >5 43.7 ± 9.2
32 Image 35 30.0 ± 6.9 >250 >8 >200
33 Image 36 35.7 ± 3.8 >250 >7 26.7 ± 7.3
34 Image 37 >50 >250 >5 17.1 ± 6.9
35 Image 38 25.8 ± 5.7 >250 >10 19.0 ± 8.4
36 Image 39 1.3 ± 0.5 >250 >192 42.9 ± 8.3
37 Image 40 2.1 ± 1.1 >250 >119 41.3 ± 7.6

All data were obtained by analysis with nonlinear regression function of GraphPad Prism 8.0.

a

50% Effective Concentration at half-maximal response, i.e., the compound concentration that inhibits 50% of plaque formation as determined by PRA against SARS-CoV-2. Reported values represent the means ± SD of data derived from n ≥ 3 independent experiments in duplicate.

b

Compound concentration that produces 50% of cytotoxicity, as determined by MTT assays at 72 h in Vero E6 cells. Reported values represent the means ± SD of data derived from n = 3 independent experiments in duplicate.

c

SI, Selectivity Index (determined as the ratio between CC50 and EC50).

d

50% Inhibitory Concentration at half-maximal response, i.e., the compound concentration that inhibits 50% of SARS-CoV-2 Mpro activity in vitro. Reported values represent the means ± SD of data derived from n ≥ 3 independent experiments in duplicate.