Table 6. Activity of IKK16 Analogues against P. falciparum Blood Stage Proliferation with the Associated Cytotoxicity against HepG2 Cells.
| compound | Pf3D7 EC50 (nM ± SEM)a | % viability@200 nMb | % viability@2 μMb |
|---|---|---|---|
| IKK16 | 280 ± 2 | 110 | 103 |
| 12 | 60 ± 5 | 100 | 97 |
| 18b | 541 ± 29 | 105 | 82 |
| 18m | 810 ± 19 | 110 | 87 |
| 18n | 760 ± 61 | 87 | 66 |
| 18o | 646 ± 10 | 83 | 55 |
| 18q | 607 ± 16 | 98 | 79 |
| 18r | 991 ± 65 | 94 | 61 |
| 18s | 300 ± 9 | 83 | 47 |
| 18t | 322 ± 7 | 95 | 84 |
| 23c | 576 ± 28 | 87 | 65 |
| 23d | 552 ± 37 | 113 | 34 |
| 23e | 1400 ± 13 | 102 | 65 |
| 23f | 2600 ± 35 | 99 | 54 |
EC50 values were determined using the SYBR green I-based assay with 2-fold dilutions, presented as mean values performed in triplicate.
% of viable cells after incubation with 200 nM and 2 μM of the test compounds, presented as an average of two experiments performed in quadruplicate.