Table 3.
The antimalarial activity of the series of novel derivatives of caffeic acid against the D10 (CQ-sensitive) and W2 (CQ-resistant) strains of P. falciparum and their cytotoxicity to NHDF cells.
| Compound | P. falciparum IC50 (μM) | RIa | Cytotoxicityb IC50 (μM) | SID10c | SIW2d | |
|---|---|---|---|---|---|---|
| D10 | W2 | |||||
| 1 | 28.63 ± 1.94 | 86.44 ± 27.45 | 3.02 | 249.83 ± 0.51 | 8.73 | 2.89 |
| 2 | 42.11 ± 9.12 | 38.78 ± 17.80 | 0.92 | 115.40 ± 1.76 | 2.74 | 2.98 |
| 3 | 12.71 ± 2.33 | 11.29 ± 4.81 | 0.89 | 79.22 ± 6.14 | 6.23 | 7.02 |
| 4 | 12.18 ± 4.90 | 10.96 ± 4.88 | 0.90 | 90.34 ± 10.32 | 7.42 | 8.24 |
| 5 | 145.08 ± 53.63 | 130.75 ± 52.71 | 0.90 | nde | — | — |
| 6 | 129.45 ± 59.63 | 117.42 ± 35.87 | 0.91 | 228.75 ± 7.57 | 1.77 | 1.95 |
| CA | >277.53 | >277.53 | — | nde | — | — |
| CQ | 0.02 ± 0.01 | 0.23 ± 0.08 | 11.5 | 40.95 ± 2.29f | 2047.5 | 178.04 |
aRatio between the IC50 values of each compound against the W2 and D10 strains of P. falciparum. bThe cytotoxic activity assayed in vitro on NHDF cells using the MTT assay. cSID10 = IC50(NHDF)/IC50 (D10). d4 SIW2 IC50 (NHDF)/IC50 (W2). eNot determined. fData taken from reference [33].