Table 1. LogD/LogP, Kinetic Solubility, in Vitro Intrinsic Clearance and Activity against P. falciparum for Ring A Variants^d.

^aValue measured using a chromatographic gLogD technique.

^bEstimated using nephelometry.

^cIn vitro intrinsic clearance determined in mouse hepatic microsomes.

^dChloroquine, EC₅₀P. falciparum K1 0.095–0.172 μM; podophyllotoxin EC₅₀ L6 cells 0.009–0.022 μM. The EC₅₀ values are the means of two independent assays and varies less than ±50%. n.d = not determined.