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. 2022 Sep 27;65(19):13172–13197. doi: 10.1021/acs.jmedchem.2c00996

Table 6. Activity of IKK16 Analogues against P. falciparum Blood Stage Proliferation with the Associated Cytotoxicity against HepG2 Cells.

compound Pf3D7 EC50 (nM ± SEM)a % viability@200 nMb % viability@2 μMb
IKK16 280 ± 2 110 103
12 60 ± 5 100 97
18b 541 ± 29 105 82
18m 810 ± 19 110 87
18n 760 ± 61 87 66
18o 646 ± 10 83 55
18q 607 ± 16 98 79
18r 991 ± 65 94 61
18s 300 ± 9 83 47
18t 322 ± 7 95 84
23c 576 ± 28 87 65
23d 552 ± 37 113 34
23e 1400 ± 13 102 65
23f 2600 ± 35 99 54
a

EC50 values were determined using the SYBR green I-based assay with 2-fold dilutions, presented as mean values performed in triplicate.

b

% of viable cells after incubation with 200 nM and 2 μM of the test compounds, presented as an average of two experiments performed in quadruplicate.