Table 4.
Structure-activity relationships of compound 24 analogsa
| |||||||
---|---|---|---|---|---|---|---|
compd | R | IC50 (nM) | cLogP | LipE | CC50 (µM) | SI | |
24 |
|
7000 | 5.5 | −0.3 | 75 | 11 | |
24a |
|
42 | 5.1 | 2.3 | 16 | 374 | |
24b |
|
46 | 4.7 | 2.7 | 26 | 570 | |
24c |
|
208 | 5.6 | 1.1 | NA | nd | |
24d |
|
244 | 5.6 | 1.0 | 36 | 152 | |
24e |
|
NA | 5.5 | nd | 27 | nd |
Antiviral IC50 and cytotoxicity CC50 values were determined from triplicate measurements and repeated at least twice. Values ≥ 100 µM were deemed not active (NA), or otherwise not determined (nd).