Table 1. In Vitro Antimalarial Activity and Toxicity of Tetraoxanes 5, 8, 10, and 12 and Trioxanes 16–18.
| in vitro
activity (IC50/nM) |
cytotoxicity (IC50/μM) | ||
|---|---|---|---|
| compd | blood-stagea | liver-stageb | Huh7 |
| 3 | 12.5c | 155c | ND |
| 5 | 21.1 | 538 | >100 |
| 8 | 45.2 | >1000 | 5.02 |
| 10 | 36.5 | 604 | 2.57 |
| 12 | 21.6 | 330 | 8.20 |
| 16 | 9.3 | >1000 | 32.8 |
| 17 | 9.1c | 523c | ND |
| 18 | 5.1 | 67 | 73.0 |
| 4, ethyl ester | 128.2 | NA | ND |
| PQ | 3300 | 7500 | ND |
| ART | 8.2 | NA | ND |
| PQ + ART | ND | 9714 | ND |
a
Determined against the chloroquine-resistant P. falciparum W2 strain.
b
Determined against P. berghei; ND, not determined; NA, not active (>10 μM).
c
Ref (23).