Table 2 In vitro antimalarial activities and cytotoxicities of DQ derivatives (determined by SYBR Green I fluorescence viability readout, data from three independent biological replicates, n = 3, each performed in technical triplicates, ±SE)
Compd | cLogP | IC50 (nM)a | Resistance indexb | IC50 (µM) WI-38c | Selectivity index SId | |||
|---|---|---|---|---|---|---|---|---|
NF54 | K1 | W2 | RI1 | RI2 | ||||
ARM | ND | 5.77 ± 1.33 | 7.26 ± 2.34 | 4.5 ± 0.78 | 1.3 | 0.8 | ND | ND |
ARS | ND | 7.88 ± 1.35 | 8.97 ± 2.26 | 6.77 ± 1.13 | 1.4 | 0.8 | >100 | >12,690 |
CQ | ND | 510 ± 3.8 | 154.7 ± 14.9 | 233.18 ± 49 | 15.0 | 22.6 | ND | ND |
DQ 2 | 8.19 | 26.6 ± 1.4 | 64.9 ± 8.8 | 15.4 ± 3.4 | 2.4 | 0.6 | >100 | >3759 |
11 | 5.5 | >200 | >200 | >200 | ND | ND | 54.9 | ND |
12 | 5.3 | 156.9 ± 10.6 | 197.7 ± 41.4 | 194.5 ± 48.3 | 1.3 | 1.2 | 41.3 | 263 |
17 | 4.7 | >200 | >200 | >200 | ND | ND | 40.1 | ND |
18 | 5.6 | >200 | >200 | >200 | ND | ND | 83.4 | ND |
21 | 5.0 | 6.8 ± 3.9 | 14.4 ± 6.3 | 5.7 ± 3.5 | 2.0 | 0.8 | >100 | >14,705 |
22 | 3.8 | 1.4 ± 0.5 | 1.3 ± 0.6 | 1.1 ± 0.1 | 0.9 | 0.7 | >100 | >71,428 |
23 | 3.5 | 93.1 ± 35.4 | 80.5 ± 34.1 | 47.1 ± 2.9 | 0.8 | 0.5 | >100 | >1074 |
24 | 2.9 | 9.6 ± 2.9 | 15.0 ± 5.6 | 7.4 ± 1.9 | 1.5 | 0.7 | >100 | >10,416 |
25 | 5.2 | 136.0 ± 41.9 | ˃200 | 84.4 ± 28.1 | 2.0 | 0.6 | >100 | >735 |
26 | 3.2 | 92.1 ± 49.3 | 65.35 ± 22.3 | 19.8 ± 1.2 | 1.2 | 0.2 | 40.1 | 435 |
27 | 2.7 | 21.9 ± 11.7 | 16.8 ± 5.9 | 9.1 ± 1.1 | 0.7 | 0.4 | 56.5 | 2579 |
Emetine | ND | ND | ND | ND | ND | ND | 0.05 | ND |
