Table 2.
Filoviral entry inhibitory activity of tetrahydronaphthalene derivatives 37–42 compared to their precursor 1,2-dihydronaphthalene (25, 27, 28, 32 and 35) against pEBOV and pMARV.
|
|||||||
|---|---|---|---|---|---|---|---|
| # | Structure | R | A549 CC50 (μM) | pEBOV EC50 (μM)a | SI pEBOVb | pMARV EC50 (μM)a | SI pMARVb |
| 25 | I |
|
8.0 ± 0.1 | 0.03 ± 0.01 | 253 | 1.1 ± 0.1 | 7 |
| 37 | II | 15.6 ± 0.3 | 0.26 ± 0.09 | 60 | 1.2 ± 0.1 | 13 | |
| 27 | I |
|
14.1 ± 0.4 | 0.04 ± 0.03 | 392 | 1.6 ± 0.1 | 9 |
| 38 | II | 57 ± 2 | 0.74 ± 0.11 | 77 | 3.3 ± 0.2 | 17 | |
| 28 | I |
|
29 ± 0.6 | 0.06 ± 0.01 | 471 | 4.1 ± 0.4 | 7 |
| 39 | II | 36 ± 1 | 0.86 ± 0.10 | 42 | 5.8 ± 2.2 | 6 | |
| 32 | I |
|
>100 | >100 | ndc | 4.9 ± 1.6 | >20 |
| 40 | II | >100 | >100 | ndc | 1.5 ± 0.1 | >66 | |
| 35 | I |
|
7.5 ± 0.1 | 0.026 ± 0.005 | 293 | 0.44 ± 0.10 | 17 |
| 41 | II | 6.8 ± 0.2 | 0.040 ± 0.002 | 172 | 0.42 ± 0.03 | 16 | |
| 42 | II |
|
8.7 ± 0.4 | 2.9 ± 0.1 | 3 | 0.60 ± 0.09 | 15 |
Dose–response curves were used to calculate EC50 values using the four-parameter variable slope nonlinear regression analysis in GraphPad Prism 10.2.3. Data are presented as the mean EC50 from three replicates ± standard deviation.
Selectivity indices are calculated as the ratio of CC50/EC50 where CC50 is cytotoxicity measured in a CellTiter-Glo Luminescent Cell Viability Assay.
Not determined.