Compound codea | CC50 (μg/mL) | SI on 3D7 | SI on Dd2 | Mean SI |
---|
1 | 187.5 | 22.17 | 32.91 | 27.54 ± 7.59 |
2 | 187.5 | 43.51 | 31.37 | 37.44 ± 8.58 |
3 | 62.5 | 19.45 | 15.16 | 17.31 ± 3.0 |
7 | 375 | 93.67 | 148.34 | 121.01 ± 38.7 |
8 | 93.75 | 21.14 | 71.67 | 46.41 ± 35.7 |
9 | 250 | 149.52 | 162.97 | 156.25 ± 9.5 |
11 | 187.5 | 74.49 | 182.03 | 128.26 ± 76.1 |
12 | 187.5 | 55.52 | 67.39 | 61.46 ± 8.39 |
13 | 375 | 63.71 | 69.70 | 66.71 ± 4.24 |
- Chemical classes of compounds:- ketones: 1–3 and alcohols: 7–12. a Compounds 4, 5, 6 and 10 not tested for cytotoxicity due to low activity in either the primary screen (< 50% inhibition) and or the secondary screen (IC50 > 10 μg/mL). Classification of cytotoxicity: CC50 < 1 μg/mL (high cytotoxicity), CC50 1 μg/mL-10 μg/mL (moderate cytotoxicity), CC50 10 μg/mL-30 μg/mL (mild cytotoxicity) and CC50 > 30 μg/mL (no observable cytotoxicity) [25]. Selectivity Index (SI) = CC50 on LLC-MK2 cells/IC50 on P. falciparum. Mean SI: geometric mean of the Selectivity Indices of the 3D7 and Dd2 parasite strains. Cut-off point for selectivity: SI > 10 (non-toxic); SI ≤ 10 (toxic) [20]