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. 2023 Jan 25;14(3):507–519. doi: 10.1039/d2md00149g

Anti-SARS-CoV-2 activity on A549-ACE2 cells (RT-qPCR) and cell cytotoxicity of the 22 compounds, expressed as EC50 in μM, the concentration at which 50% inhibition of the maximal signal is observed at 95% confidence interval.

graphic file with name d2md00149g-u1.jpg
Entry R1 R2 Saturation on the LHS RT-qPCR Beta EC50 (μM) [95% CI] Cytotoxicity CC50 (μM) [95% CI] Ratio cytotoxicity/RT-qPCR
3a′ graphic file with name d2md00149g-u2.jpg Double bond 16 (N/A) 14 [2.8 to 73] 0.9
3a graphic file with name d2md00149g-u3.jpg H Double bond 17 [13 to 23] >50 >3
3b′ graphic file with name d2md00149g-u4.jpg Double bond 13 [7.2 to 24] 6.6 [2.7 to 16] 0.5
3b graphic file with name d2md00149g-u5.jpg H Double bond 3.7 [2.0 to 6.9] 3.5 [2.3to 5.6]a 12 [10 to 15] 3.3
>50a
3c graphic file with name d2md00149g-u6.jpg H Double bond 8.3 [6.3 to 11] 13 (N/A) 1.6
5 H Saturated >50 >50 N/A
6 Me Saturated >50 >50 N/A
7 graphic file with name d2md00149g-u7.jpg Saturated 8.4 [5.5 to 13] 5.8 [3.0 to 11] 0.7
8a graphic file with name d2md00149g-u8.jpg H Saturated 16 [5.2 to 51] >50 >3
8b graphic file with name d2md00149g-u9.jpg H Saturated 14 [8.5 to 22] 20 [8.2 to 48] 1.4
8c graphic file with name d2md00149g-u10.jpg H Saturated 37 [23 to 59] >50 1.4
8d′ graphic file with name d2md00149g-u11.jpg Saturated 5.3 [4.0 to 7.1] 37 N/A 6.9
8d graphic file with name d2md00149g-u12.jpg H Saturated 6.6 [4.3 to 10] 12 [6.7 to 21] 1.6
8e graphic file with name d2md00149g-u13.jpg H Saturated 5.6 N/A 13 [7.6 to 21] 2.3
8f graphic file with name d2md00149g-u14.jpg H Saturated >50 >50 N/A
8h graphic file with name d2md00149g-u15.jpg H Saturated >17 >50 N/A
9a graphic file with name d2md00149g-u16.jpg graphic file with name d2md00149g-u17.jpg Saturated >40 [N/A] >50 [N/A] N/A
9b graphic file with name d2md00149g-u18.jpg graphic file with name d2md00149g-u19.jpg Saturated 6.2 [N/A] 6.3 [3.7 to 11] 1.0
9c Me graphic file with name d2md00149g-u20.jpg Saturated 20 [N/A] 17 [14 to 18] 0.8
9d graphic file with name d2md00149g-u21.jpg graphic file with name d2md00149g-u22.jpg Saturated >50 >50 N/A
9e graphic file with name d2md00149g-u23.jpg graphic file with name d2md00149g-u24.jpg Saturated 1.4 [0.9 to 2.2] 4.4 [2.0 to 9.0]a 7.7 [5.2 to 12] 5.7
>20a
10 graphic file with name d2md00149g-u25.jpg graphic file with name d2md00149g-u26.jpg Double bond >50 N/A
a

Assays against cells infected with SARS-CoV-2 variant Omicron BA1.