Table 1. Biological Activity and Cytotoxicity Data of Synthesized Compounds 9a–i, 10a–h, and 11a–da.
| 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 |
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.