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Preliminary SAR of Triazole Thioether Scaffold
| Compound |
 |
HIV/EBOV-GP |
||||
|---|---|---|---|---|---|---|
| R1 | R2 | R3 | IC90, µmol/L | CC50, µmol/L | SI | |
| MBX2270 | 4-OEt | Ph |  |
25.7 | >50 | ND |
| 7 846 036 | 3-CF3 | Ph |  |
6.3 | 55 | 9 |
| 7 629 169 | 2-Cl | Ph |  |
2.5 | 21 | 8 |
| 7 909 196 | 2-CF3 | 4-Tol |  |
82 | >100 | ND |
| 7 682 333 | 3,4-diMe | Et |  |
6.3 | 35 | 6 |
Abbreviations: CC50, 50% cytotoxic concentration; HIV/EBOV-GP, Ebola pseudotype; IC90, 90% inhibitory concentration; ND, not determined; SAR, structure activity relationship; SI, selectivity index.
