Table 1 Cross-resistant dose-response for the active epi-drugs. Compounds were screened for IC50 against 3D7, K1 and W2 asexual parasite strains using the SYBR Green I-based fluorescence assay. The resistance index (RI; italic) and selectivity index (SI) for each compound is shown. Compounds with SI > 10 are in bold. Results for all compounds are representative of three independent biological replicates with technical triplicates (n = 3, IC50 ± SEM).

From: Epigenetic inhibitors target multiple stages of Plasmodium falciparum parasites

Compound name

3D7

IC50 (μM) against P. falciparum strains

IC50 human cell line (μM)a

SI (based on 3D7 IC50)

K1

W2

 

RI (K1/3D7)

 

RI (W2/3D7)

3-Deazaneplanocin A

0.0117 ± 0.0023

0.007 ± 0.004

0.60

0.0358 ± 0.0032

3.06

0.19

16

BIX01294

0.028 ± 0.006

0.047 ± 0.007

1.68

0.045 ± 0.006

1.61

11

393

UNC0638

0.0283 ± 0.0032

0.039 ± 0.005

1.38

0.05 ± 0.01

1.77

23

812

HC Toxin

0.035 ± 0.013

0.019 ± 0.004

0.54

0.0291 ± 0.0016

0.83

0.037

1

TSA

0.078 ± 0.008

0.066 ± 0.008

0.85

0.066 ± 0.005

0.85

0.2

2.6

ITF2357

0.17 ± 0.01

0.122 ± 0.028

0.72

0.178 ± 0.015

1.05

0.2

1.2

4-iodo-SAHA

0.30 ± 0.07

0.40 ± 0.05

1.33

0.27 ± 0.05

0.90

1.1

3

SB939

0.32 ± 0.11

0.44 ± 0.10

1.38

0.30 ± 0.04

0.94

1.48

5

CAY10603

0.37 ± 0.08

0.367 ± 0.028

0.99

0.428 ± 0.023

1.16

10.8

29

M344

0.51 ± 0.08

0.29 ± 0.04

0.57

0.53 ± 0.04

1.04

2.3

4.6

Pyroxamide

0.51 ± 0.14

0.50 ± 0.07

0.98

0.64 ± 0.15

1.25

SAHA

0.71 ± 0.12

0.37 ± 0.04

0.52

0.43 ± 0.06

0.61

5

7

CAY10398

0.726 ± 0.005

0.2723 ± 0.0032

0.38

0.363 ± 0.030

0.50

Sinefungin

0.94 ± 0.04

1.43 ± 0.16

1.52

0.949 ± 0.032

1.01

Ellagic acid

1.9 ± 0.5

2.4 ± 1.2

1.26

3.25 ± 0.19

1.71

45

23.7

Tenovin-6

2.3 ± 0.4

4.33 ± 0.32

1.88

4.9 ± 1.2

2.13

6.09

2.65

Suberohydroxamic acid

2.77 ± 0.18

5.8 ± 0.7

2.09

2.2 ± 0.6

0.79

50

18

CBHA

3.2 ± 0.7

1.9 ± 0.3

0.59

0.77±0.04

0.24

1.8

0.56

Oxamflatin

3.7 ± 0.9

4.7 ± 1.2

1.27

2.3 ± 0.6

0.62

0.25

0.07

  1. aActivity data of the compounds on various mammalian lines were collated from previous reports15,49,65,66,67,68.