Table 2. Selected anti-plasmodium lead compounds with associated biochemical and cell-based assay data.
IC50 (µM) | Ki (µM) | GI50 (µM) | Cytotoxicity (% inhibition at 10 µM) | ||||||
cmpd | R1 | R2 | R3 | falcipain-2 | falcipain-3 | catL | catB | P. falc. W2 | Jurkat cells |
14a | furyl | furyl | — | 0.020 | 0.029 | 0.076 | 16 | 1.5 | <5% |
14b | o-ClPh | H | — | 0.0087 | 0.023 | 0.71 | 1.3 | 2.0 | <5% |
14c | H | p-MeOPh | — | 0.018 | 0.025 | 0.35 | 4.2 | 2.7 | <5% |
14d | Cl | furyl | — | 0.017 | 0.014 | 0.28 | 18 | 3.9 | <5% |
15a | — | — | CF3 | 0.050 | 0.015 | 0.15 | 54 | 3.5 | <5% |
15b | — | — | Ph | 0.024 | 0.0052 | 0.11 | 90 | >20 | <5% |