Table 2.
Activities of amino-artemisinins in vitro against early and late blood stage P. falciparum NF54 gametocytesa.
| Compounda | Early Stage (EG, Luc 48 h) IC50 nMb | Late Stage (LG, Luc 72 h) IC50 nMc | Fold change preference ratio: EG to LG | Fold change preference ratio: LG to EG |
|---|---|---|---|---|
| MBd | 95.0 ± 11.3 | 143.0 ± 16.7 | 1.5 | 0.7 |
| DHA 2d | 43.0 ± 3.9 | 33.66 ± 1.98 | 0.78 | 1.3 |
| Artemiside 7d | 16.4 ± 1.0 | 1.5 ± 0.5 | 0.09 | 10.9 |
| Artemisone 8d | 1.94 ± 0.11 | 42.4 ± 3.3 | 21.9 | 0.05 |
| DHA-piperazine 9d | 54.91 ± 5.11 | 25.7 ± 17.5 | 0.47 | 2.1 |
| Phenylurea 10d | 83 ± 2 | 1.70 ± 0.99 | 0.02 | 48.8 |
| Sulfamide 11d | 15.0 ± 2.0 | 419.4 ± 59.5 | 28.0 | 0.04 |
| Arylamine 12d | 38.2 ± 9.0 | 16.42 ± 6.38 | 0.4 | 2.3 |
| DHA piperazine sulfonamides | ||||
| 13 | 21.5 ± 10.4 | 0.5 ± 0.3 | 0.02 | 40.55 |
| 15 | 8.0 ± 2.3 | 0.9 ± 0.5 | 0.11 | 8.78 |
| 16 | 19.7 ± 9.9 | 0.4 ± 0.3 | 0.02 | 46.26 |
| 17 | 13.1 ± 7.2 | 0.6 ± 0.4 | 0.05 | 20.98 |
| 18 | 89.7 ± 28.8 | 4.8 ± 4.2 | 0.05 | 18.60 |
| 19 | 12.1 ± 4.5 | 0.7 ± 0.5 | 0.06 | 16.28 |
| DHA piperazine ureas | ||||
| 22 | 45.9 ± 9.9 | 17.7 ± 15.1 | 0.39 | 2.12 |
| 23 | 20.0 ± 9.4 | 1.0 ± 0.3 | 0.05 | 19.48 |
| 24 | 36.0 ± 10.2 | 17.0 ± 7.0 | 0.47 | 2.59 |
| DHA piperazine amides | ||||
| 27 | 43.7 ± 5.1 | 2.8 ± 1.8 | 0.06 | 33.13 |
| 28 | 19.5 ± 8.5 | 0.6 ± 0.3 | 0.03 | 15.69 |
| DHA sulfamides | ||||
| 29 | 24.7 ± 4.9 | 0.04 ± 0.03 | 0.00 | 578.76 |
| 30 | 19.3 ± 6.2 | 4.0 ± 3.8 | 0.21 | 4.77 |
b
Early stage (>90% stage I–III).
c
Late stage (>90% stage IV and V) gametocytes determined using the luciferase based assay against the Luc reporter cell line. Results are representative of the mean of three independent biological replicates, performed as technical triplicates, ±SEM. Data are from a 72-h incubation period.
d
Data from Coertzen et al. (2018).