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Table 1 Results of biological evaluation

From: Antiplasmodial dihetarylthioethers target the coenzyme A synthesis pathway in Plasmodium falciparum erythrocytic stages

ID

% inhibition, PfNF54-Luc at 3 µM

IC50 [µM], Pf3D7 + solvent

IC50 [µM], Pf3D7 + 0.8 mM CoA

IC50-ratio (CoA/solvent)

IC50 [µM], THP-1

IC50 [µM], HEK-293

3a

80.8 ± 0.5

0.283 ± 0.073

4.61 ± 0.15

16.3

6.13

>10

3b

25.7 ± 2.0 at 30 µM

nd

nd

nd

nd

3c

37.3 ± 3.7 at 30 µM

nd

nd

nd

nd

3d

−0.6 ± 5.4

nd

nd

nd

nd

3e

−7.3 ± 6.9

nd

nd

nd

nd

3f

1.5 ± 4.3

nd

nd

nd

nd

3g

−13.1 ± 9.1

nd

nd

nd

nd

3h

−103.3 ± 4.4

nd

nd

nd

nd

3i

−5.5 ± 3.8

nd

nd

nd

nd

3j

−11.0 ± 6.7

nd

nd

nd

nd

3k

−7.0 ± 1.8

nd

nd

nd

nd

3l

24.3 ± 3.2

nd

nd

nd

nd

3m

−8.3 ± 4.1

nd

nd

nd

nd

3n

−0.82 ± 3.11

nd

nd

nd

nd

3o

2.28 ± 3.31

nd

nd

nd

nd

3p

−14.6 ± 12.9

nd

nd

nd

nd

3q

−12.3 ± 2.2

nd

nd

nd

nd

3r

7.7 ± 1.8

nd

nd

nd

nd

3s

−2.8 ± 16.6

nd

nd

nd

nd

6a

−24.8 ± 13.6

nd

nd

nd

nd

6b

1.79 ± 2.53

nd

nd

nd

nd

6c

0.98 ± 1.52

nd

nd

nd

nd

8a

33.2 ± 6.8

10.5 ± 1.1

16.1 ± 2.2

1.53

nd

>40

8b

4.7 ± 2.6

5.37 ± 1.0

39.7 ± 0.7

7.39

nd

>40

8c

96.5 ± 1.6

1.26 ± 0.16

2.31 ± 0.17

1.83

>300

>40

8d

99.9 ± 0.0

0.0388 ± 0.0010

2.61 ± 0.42

67.3

27.5

>10

8e

99.5 ± 0.5

0.0747 ± 0.021

2.58 ± 0.42

34.5

33.6

>10

8f

99.7 ± 0.1

0.0958 ± 0.0063

11.2 ± 2.6

117

11

>4

8g

95.0 ± 1.1

0.0734 ± 0.0022

0.531 ± 0.007

7.23

16.5

>10

8h

−1.9 ± 5.3

nd

nd

nd

nd

8i

−18.4 ± 10.6

nd

nd

nd

nd

8j

−36.3 ± 10.6

nd

nd

nd

nd

8k

98.0 ± 0.2

0.149 ± 0.021

1.06 ± 0.03

7.11

28

>20

BS

99.3 ± 0.7

nd

nd

nd

nd

Amb 180,780

nd

0.0370 ± 0.0017

1.51 ± 0.19

40.8

nd

>40

Chloroqu

nd

0.0195 ± 0.0034

0.0271 ± 0.0094

1.39

nd

>40

Artemis

nd

0.00337 ± 0.00065

0.00490 ± 0.0011

1.45

nd

nd

Puromyc

nd

0.0338 ± 0.012

0.0939 ± 0.0016

2.78

nd

0.36

Pantoth

nd

752 ± 82

>10,000

>13.3

nd

nd

  1. nd not determined