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. 2021 May 11;6(20):12984–12994. doi: 10.1021/acsomega.0c06053

Table 1. Biological Activity and Cytotoxicity Data of Synthesized Compounds 9ai, 10ah, and 11ada.

          selectivity index (SI)
s. no. compounds code IC50Pf3D7 (μM) IC50PfK1 (μM) cytotoxicity CC50 (μM) in VERO cell line Pf3D7 PfK1
1 9a 0.06 ± 0.0 0.26 ± 0 36.57 610 61
2 9b 1.16 ± 0.26 1.19 ± 0.53 50.77 44 43
3 9c 0.15 ± 0.14 0.42 ± 0.23 69.52 463 166
4 9d 0.08 ± 0.0 0.18 ± 0.15 47 588 261
5 9e 0.23 ± 0.10 0.54 ± 0.03 60.28 262 112
6 9f 2.72 ± 1.44 2.25 ± 0.77 68.62 25 30
7 9g 2.0 ± 0.06 2.04 ± 0.40 42.63 21 21
8 9h 1.24 ± 0.0 1.60 ± 0.91 51.95 42 33
9 9i 3.80 ± 1.05 2.5 ± 1.03 51.37 14 21
10 10a 1.20 ± 0.78 1.38 ± 0.07 33.50 28 24
11 10b 0.28 ± 0.13 0.49 ± 0.15 69.69 348 142
12 10c 0.06 ± 0.16 0.10 ± 0.5 57.79 963 577
13 10d 0.21 ± 0.11 0.33 ± 0.06 79.05 376 240
14 10e 3.89 ± 0.50 ND ND NA NA
15 10f 1.37 ± 0.52 ND ND NA NA
16 10g 0.68 ± 0.16 1.77 ± 0.0 39.21 58 22
17 10h 1.75 ± 0.16 ND ND NA NA
18 11a 0.04 ± 0.0 0.06 ± 0.04 106.91 274 1782
19 11b 0.19 ± 0.0 0.11 ± 0.07 80.22 422 729
20 11c 0.88 ± 0.28 0.82 ± 0.06 >200 >227 >243
21 11d 0.09 ± 0.02 0.31 ± 0.15 78.22 978 252
22 chloroquine (reference drug) 0.003 ± 0.25 0.795 ± 0.15 513 171 000 645
a

Parasite inhibition experiment was performed in chloroquine-sensitive strain (3D7, MRA-151) and multidrug-resistant strain (K1, MRA-159). Cytotoxicity experiment was performed in VERO cells. IC50 and CC50 are the half-maximal inhibitory and cytotoxic concentrations, respectively. Chloroquine (CQ), was used as a reference compound in the parasite inhibition assay. Podophyllotoxin is used as a reference compound for cytotoxicity in VERO cells (CC50 4 μM). Selectivity index (SI) is calculated as the ratio of CC50/IC50.