From: In vitro activity of salinomycin and monensin derivatives against Trypanosoma brucei
T. brucei | HL-60 | Selectivity | ||||
---|---|---|---|---|---|---|
Compound | MIC (μM)a | GI50 (μM)b | MIC (μM)a | GI50 (μM)b | MIC ratioc | GI50 ratiod |
Salinomycin | 1 | 0.18 ± 0.06 | 1 | 0.44 ± 0.21 | 1 | 2.4 |
SAL-E1 | 10 | 3.08 ± 0.18 | 100 | 35.5 ± 2.4 | 10 | 11.4 |
SAL-E2 | 10 | 3.25 ± 0.26 | 100 | 34.6 ± 1.9 | 10 | 10.6 |
SAL-E3 | 10 | 3.10 ± 0.21 | 100 | 33.8 ± 3.5 | 10 | 10.9 |
SAL-E4 | 10 | 3.12 ± 0.08 | 100 | 32.9 ± 2.5 | 10 | 10.5 |
SAL-E5 | 10 | 3.21 ± 0.02 | 100 | 38.4 ± 4.2 | 10 | 11.0 |
SAL-E6 | 10 | 3.01 ± 0.06 | > 100 | > 100 | > 10 | > 33 |
SAL-E7 | 0.1–1e | 0.057 ± 0.029 | 100 | 16.4 ± 1.9 | 100–1000 | 288 |
SAL-AM1 | 10 | 3.23 ± 0.21 | 100 | 38.9 ± 3.2 | 10 | 12.0 |
SAL-AM2 | 0.1 | 0.040 ± 0.007 | 100 | 14.5 ± 1.3 | 1000 | 363 |
SAL-AM3 | 10 | 2.94 ± 0.20 | 100 | 7.92 ± 1.95 | 10 | 2.7 |
SAL-AM4 | 10 | 2.69 ± 0.51 | 100 | 24.5 ± 3.7 | 10 | 9.1 |
SAL-AM5 | 10 | 2.69 ± 0.20 | 100 | 39.2 ± 1.6 | 10 | 14.6 |
Monensin | 0.1 | 0.029 ± 0.002 | 10 | 1.48 ± 0.56 | 100 | 51 |
MON-E1 | 10 | 3.06 ± 0.06 | 100 | 34.1 ± 2.2 | 10 | 11.1 |
MON-E2 | 10 | 2.76 ± 0.10 | 100 | 25.3 ± 5.0 | 10 | 9.2 |
MON-E3 | 10 | 1.68 ± 0.56 | 100 | 20.3 ± 3.1 | 10 | 12.1 |
MON-UR1 | 1 | 0.31 ± 0.06 | 100 | 23.3 ± 6.6 | 100 | 75 |
Suraminf | 0.1 | 0.035 ± 0.002 | > 100 | > 100 | > 1000 | > 2857 |