Table 3.
In vitro Activity of Investigated Malaria Box Compounds Against Asexual Blood Stages of W2, CQ-R, and 3D7, CQ-S P. falciparum Strains and Comparison with Data in the Literature
Compound Name | P. falciparum Asexual Blood Stages IC50 (µM) | |||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
CQ-Resistant Strains | CQ-Sensitive Strains | |||||||||||||
W2a | Dd2b | W2b | K1b | K1c | Dd2d | FCR3e | 3D7a | 3D7b | HB3b | 3D7f | 3D7f | 3D7f | 3D7g | |
1. MMV000662 | 0.133±0.069 | 0.053 | 0.049 | 0.066 | 0.074 | 1.258 | 0.120±0.050 | 0.049 | 0.058 | 0.262 | 0.37 | 0.343 | 0.037 | |
2. MMV006429 | 0.132±0.038 | 0.073 | 0.077 | 0.079 | 0.039 | 0.16 | 0.074 | 0.123±0.003 | 0.062 | 0.213 | 0.385 | 0.3 | 0.033 | |
3. MMV000642 | 0.070±0.002 | 0.051 | 0.046 | 0.117±0.012 | 0.02 | |||||||||
4. MMV019266 | > 8 | 0.079 | 0.062 | 0.153 | 0.582 | 0.844 | 0.044 | >8 | 0.058 | 0.093 | 0.62 | |||
5. MMV665876 | 0.690±0.048 | 0.078 | 0.06 | 0.123 | 0.916 | 0.338 | 0.158 | 0.340±0.016 | 0.129 | 0.15 | 0.181 | 0.415 | 0.26 | |
6. MMV006767 | 2.148±0.031 | 0.357 | 0.797 | 1.494 | 0.884 | 0.931 | 1.020±0.319 | 0.592 | 0.812 | 0.93 | ||||
7. MMV085583 | 0.101±0.036 | 0.245 | 0.147 | 0.082 | 0.288 | 0.179 | 0.179 | 0.171±0.045 | 0.165 | 0.200 | 0.129 | 0.144 | 0.24 | |
8. MMV665827 | 0.295±0.018 | 0.063 | 0.259 | 0.276 | 0.173±0.005 | 0.165 | 0.130 | 0.12 | ||||||
DHA | 0.002±0.001 | 0.002±0.001 | ||||||||||||
CQ | 0.304±0.138 | 0.022±0.006 |
Notes: aOriginal data from this work. Mean ± SD of at least two experiments. b–g Data were generated in the laboratories of Ayong, Avery, Horrocks, Van Voorhis and Poulsen and published as original data in the review of Van Voorhis et al; Creative Commons CCO public domain dedication.10
Abbreviations: CQ, chloroquine; DHA, dihydroartemisinin.