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. 2016 Feb 10;2(4):281–293. doi: 10.1021/acsinfecdis.5b00143

Figure 4.

Figure 4

DOS compounds exhibit stereoselective inhibition of Pb-Luc exoerythrocytic-stage parasite growth. (a) Representative compounds and activity profiles with activity against P. berghei in HepG2 cells. Stereocenters (Cn) are listed below the corresponding chemical structure. Pb-Luc exoerythrocytic-stage activity was measured for each of the eight possible stereoisomers (SRR, SSR, SRS, SSS, RRR, RSR, RRS, and RSS) of each compound. Three of the eight possible stereoisomers of BRD9781 have exoerythrocytic-stage activity, two with potent activity (SRR and SSS, IC50 < 0.1 μM) and another with moderate activity (RSS, IC50 < 1 μM). One stereoisomer of BRD0326 (SSS) is active (IC50 < 1 μM). Two stereoisomers of BRD47390 have significant exoerythrocytic-stage activity (SSR, IC50 < 0.1 μM; SRS, IC50 < 0.1 μM). (b) Compounds were tested in dose in the P. berghei/HepG2 assay, a Dd2 erythrocytic-stage assay, and in a mammalian cell cytotoxicity assay. Compounds from three scaffold libraries are shown. Compounds were tested twice in the exoerythrocytic-stage assay; values from the second assay are shown in parentheses.