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Table 3 CC50s and selectivity indices of piperidine analogues on LLC-MK2 monkey kidney epithelial cells

From: Structurally simple synthetic 1, 4-disubstituted piperidines with high selectivity for resistant Plasmodium falciparum

Compound codea

CC50 (μg/mL)

SI on 3D7

SI on Dd2

Mean SI

1

187.5

22.17

32.91

27.54 ± 7.59

2

187.5

43.51

31.37

37.44 ± 8.58

3

62.5

19.45

15.16

17.31 ± 3.0

7

375

93.67

148.34

121.01 ± 38.7

8

93.75

21.14

71.67

46.41 ± 35.7

9

250

149.52

162.97

156.25 ± 9.5

11

187.5

74.49

182.03

128.26 ± 76.1

12

187.5

55.52

67.39

61.46 ± 8.39

13

375

63.71

69.70

66.71 ± 4.24

  1. Chemical classes of compounds:- ketones: 1–3 and alcohols: 712. a Compounds 4, 5, 6 and 10 not tested for cytotoxicity due to low activity in either the primary screen (< 50% inhibition) and or the secondary screen (IC50 > 10 μg/mL). Classification of cytotoxicity: CC50 < 1 μg/mL (high cytotoxicity), CC50 1 μg/mL-10 μg/mL (moderate cytotoxicity), CC50 10 μg/mL-30 μg/mL (mild cytotoxicity) and CC50 > 30 μg/mL (no observable cytotoxicity) [25]. Selectivity Index (SI) = CC50 on LLC-MK2 cells/IC50 on P. falciparum. Mean SI: geometric mean of the Selectivity Indices of the 3D7 and Dd2 parasite strains. Cut-off point for selectivity: SI > 10 (non-toxic); SI ≤ 10 (toxic) [20]