Table 2 In vitro antimalarial activity and interaction with hemin, inhibition of β-hematin formation
Compound | Interaction with hemin | Inhibition of β-hematin formation | ||||
|---|---|---|---|---|---|---|
3D7(nM)a | W2(nM)a | Log Kd | IR | HAI50(mM) in buffere | HAI50(mM) in interfacef | |
(1) Au(CQ)(Cl) | 10 (1.80) | 483 (0.84) | 4.76 ± 0.20 | + | 0.82 ± 0.04 (0.2) | 0.99 ± 0.08 (2.3) |
(2) Au(CQ)(TaTg) | 15 (1.20) | 175 (2.32) | 4.63 ± 0.03 | + | 0.75 ± 0.05 (0.2) | 2.32 ± 0.11 (0.9) |
(3) Pt(CQDP)2(Cl)2 | 7 (2.57) | 89 (4.56) | 4.89 ± 0.10 | + | 1.88 ± 0.11 (0.1) | 2.09 ± 0.61 (1.1) |
(4) Pt(CQDP)2(I)2 | 10 (1.80) | 177 (2.29) | 4.85 ± 0.09 | + | 0.52 ± 0.06 (0.3) | 1.86 ± 0.06 (1.2) |
(5) Pd(CQ)2(Cl)2 | 12 (1.50) | 653 (0.62) | 4.09 ± 0.04 | + | 0.46 ± 0.02 (0.3) | 1.88 ± 0.81 (1.2) |
(6) Pd(CQDP)2(I)2 | 24 (0.75) | 608 (0.67) | 4.45 ± 0.02 | + | 0.34 ± 0.08 (0.4) | 2.21 ± 0.12 (1.0) |
CQDP | 18 (−−) | 406 (−−) | 5.01 ± 0.01 | + | 0.15 ± 0.03 (1) | 2.23 ± 0.09 (1.0) |