Table 1 Inhibitory activity of the 4,5-diaryl 2H-1,2,3-triazoles, 4-carboxylate-5-aryl-2H-1,2,3-triazoles and 4-carboxamide-5-aryl-2H-1,2,3-triazoles against purified human IDO1 enzyme.

From: 4,5-Disubstituted 1,2,3-triazoles: Effective Inhibition of Indoleamine 2,3-Dioxygenase 1 Enzyme Regulates T cell Activity and Mitigates Tumor Growth

Substituents

Compound 1

Compound 2

Compound 3

R1

R2

 

hIDO1

IC50 (µM)a

 

hIDO1

IC50 (µM)a

 

hIDO1

IC50 (µM)a

H

H

1a

90.033 ± 2.942

2a

14.390 ± 3.357

3a

8.541 ± 0.084

H

Me

1b

54.871 ± 0.757

2b

1.699 ± 0.061

3b

7.082 ± 0.691

F

H

1c

4.991 ± 0.057

2c

31.440 ± 4.207

3c

6.611 ± 0.355

Cl

H

1d

2.513 ± 0.060

2d

2.550 ± 0.033

3d

2.687 ± 0.055

Br

H

1e

21.870 ± 1.270

2e

2.981 ± 0.012

3e

26.680 ± 2.199

H

F

1f

25.240 ± 1.703

2f

8.090 ± 0.210

3f

2.941 ± 0.034

H

Cl

1g

3.208 ± 0.100

2g

0.392 ± 0.084

3g

0.624 ± 0.023

H

Br

1h

40.720 ± 2.696

2h

18.450 ± 1.676

3h

5.156 ± 0.011

F

F

1i

7.721 ± 0.761

2i

0.545 ± 0.029

3i

0.111 ± 0.005

Cl

Cl

1j

12.910 ± 0.191

2j

0.163 ± 0.025

3j

0.069 ± 0.004

Cl

F

1k

6.913 ± 0.099

2k

1.691 ± 0.102

3k

1.831 ± 0.126

Br

F

1 l

1.935 ± 0.083

2 l

3.035 ± 0.091

3 l

1.993 ± 0.005

  1. ahIDO1 IC50 values are the mean of three independent assays.