Table 2. In vitro activity of the compounds against asexual stages, mature gametocytes and assessment of cytotoxicity in the HepG2 cell line.

Compounds	IC50 (µM)
	Activity against asexual forms (3D7A)	Activity against asexual forms (3D7HT-GFP)	Activity against mature gametocytes IV–V	Cytotoxicity
Quinolines
Chloroquine	0.006±0.0002	0.007±0.002	23.47±2.66	51.84±7.86
Primaquine	>10	>10	20.90±4.65	>50
Isoquine	0.009±0.0016	0.0044±0.0032	28.5±2.12	17.07±6.3
Pyronaridine	0.0045±0.0015	0.00080±0.0001	3.25±0.92	5.95±0.92
Artemisinin Endoperoxides
Artesunate	0.037±0.025	0.054±0.03	10.83±3.7	>50
Dihydroartemisinin	0.0028±0.0007	0.013±0.003	3.56±0.95	>50
Amino alcohols
Quinine	0.066±0.018	0.106±0.040	>50	>50
Mefloquine	0.026±0.017	0.028±0.0014	4.70±2.10	11±0.26
Lumefantrine	0.0032±0.00014	0.00165±0.00007	>50	>50
Halofantrine	0.0011±0.0005	0.0012±0.0005	6.70±0.42	>50
DHFR-TS inhibitors
Pyrimethamine	0.0025±0.0009	33.66±6.72*	>50	>50
Hydroxy-naphthoquinones
Atovaquone	0.0007±0.0004	0.0018±0.0002	16.10±2.12	>40a
Proteasome inhibitors
Epoxomicin	0.008±0.001	0.0098±0.0017	0.00042±0.00011	0.003±0.0005
Dyes
Methylene blue	0.011±0.008	0.010±0.0018	0.49±0.16	6.52±1.31
Protein synthesis inhbitors
Azythromycin	>10	>10	28.45±0.64	>50
Cycloheximide	0.198±0.0017	0.194±0.0077	6.23±2.46	2.95±0.35

Inhibition of uptake of a radiolabeled nucleic acid precursor by the parasites served as the indicator of antimalarial activity against asexual stages while the activity on mature gametocytes was determined with the ATP bioluminescence assay. Finally, cytotoxicity was assessed using the short-term resazurin-based reductase assay. All the results are expressed as the average value of the IC₅₀ ± standard deviation (3–6 independent experiments).

^alimit of solubility.

^*resistance to pyrimethamine due to a selection cassette in the episome (containing the GFP gene).