From: Inhibitors of ubiquitin E3 ligase as potential new antimalarial drug leads
Compound Name | P. falciparum D6 (CQ-sensitive strain) IC50 (μM) | P. falciparum W2 (CQ-resistant strain) IC50 (μM) | Vero Cell Cytotoxicity a | THP1 Cell Cytotoxicity d | ||||||
---|---|---|---|---|---|---|---|---|---|---|
 | 48 h | 72 h | 96 h | 120 h | 48 h | 72 h | 96 h | 120 h | 48 h | 48 h |
Chloroquine | 0.03 ±0.001 | 0.02 ±0.004 | 0.02 ±0.001 | 0.02 ±0.001 | 0.19 ±0.004b **** | 0.19 ±0.007 b *** | 0.20 ±0.001 b **** | 0.19 ±0.002 b *** | NC | NC |
Thalidomide | NA | NA | NA | NA | NA | NA | NA | NA | NC | NC |
proTAME | NA | NA | NA | NA | NA | NA | NA | NA | NC | NC |
NSC 66811 | 32.18 ±4.57 | 37.02 ±1.80 | NA | NA | 28.74 ±4.01 | 38.95 ±2.71 | NA | NA | NC | 37.8 ±4.1 |
Nutlin 3 | 12.76 ±1.34 | 19.43 ±0.34 | 15.93 ±1.24 | 20.02 ±4.52 | 18.56 ±1.6 | 15.72 ±0.04 | 15.44 ±0.54 | 15.59 ±2.17 | NC | 35.2 ±2.76e f## |
HLI 373 | 2.36 ±0.05 | 3.07 ±0.04 | 2.98 ±0.01 | 2.43 ±0.25 | 3.47 ±0.02 b * | 4.81 ±0.41 b ** | 4.74 ±0.09 b ** | 4.04 ±0.04 b ** | NC | 23.2 ±0.07 e f ### |
JNJ 26854165 | 2.17 ± 0.004 | 2.93 ± 0.03 | 1.41 ±0.03 | 1.46 ±0.12 | 1.86 ±0.03 | 1.74 ±0.27 b * | 2.28 ±0.03 | 2.02 ±0.36 | 26.9 8 ± 1.96c | 22.4 ±0.56 e f ### |
SMER 3 | 12.06 ± 0.68 | 49.04 ±0.94 | NA | NA | 20.58 ±5.19 | 23.69 ±3.53 b * | 45.80 ±0.09 | 48.58 ±0.49 | 16.0 ±0.55 | 5.8 ±0.28 f # |
NSC 146109 | 5.24 ± 0.20 | 4.80 ±0.05 | 3.09 ±0.08 | 2.52 ±0.39 | 2.07 ±0.22 b **** | 2.63 ± 0.05 b *** | 2.91 ±0.03 | 3.23 ±0.03 | 5.27 ±0.05 | 1.2 ±0.28 |