Table 1 Cytotoxicity of OSM-S-106 and derivatives against P. falciparum (3D7) and the HepG2 mammalian cell line

From: Reaction hijacking inhibition of Plasmodium falciparum asparagine tRNA synthetase

Compound

OSM-S-106

OSM-E-32

OSM-S-137

OSM-S-488

OSM-LO-80

OSM-LO-81

OSM-LO-87

OSM-LO-88

Pf3D7

IC50(72 h) (μM)

0.058 ± 0.017

(n = 8)

8.3/8.3

(n = 2)

4.4 ± 3.0

(n = 4)

12.7/13.8

(n = 2)

5.1 ± 3.2

(n = 8)

0.93 ± 0.24

(n = 6)

>25

(n = 6)

18.7 ± 1.8

(n = 6)

HepG2

IC50(72 h) (μM)

49.6/47.3 (n = 2)

N/A

N/A

N/A

17.2/18.2 (n = 2)

43.4/43.9

(n = 2)

N/A

N/A

P. berghei liver stage IC50(72 h) (μM)

0.25/0.42

(n = 2)

N/A

N/A

N/A

N/A

N/A

N/A

N/A

  1. n = number of biological repeats. Where available, data are expressed as mean ± SD.