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Table 1 IC50 inhibition of COX1 and COX2, Selectivity ratio for COX1/COX2, and the CC50 on HeLa cancer cell line of the synthesized compounds

From: Design, synthesis and biological evaluation of novel benzodioxole derivatives as COX inhibitors and cytotoxic agents

The IC50 in µM of COX 1 and COX2

COX1/COX2 Ratio

HeLa Cell CC50 in milli-molar

Codes

X

R1

R2

R3

COX1

COX2

Selectivity

CC50

3a

O-CH3

H

H

H

12.320

14.340

0.859

1.49

3b

O-CH3

I

H

H

1.120

1.300

0.862

0.228

3c

O-CH3

H

I

H

27.060

37.450

0.723

1.79

3d

O-CH3

Br

H

H

1.3

1.45

0.897

1.61

3e

O-CH3

H

Br

H

2.360

2.730

0.864

0.219

3f

O-CH3

Cl

H

Cl

5.180

4.100

1.263

0.949

4a

OH

H

H

H

1.450

3.340

0.434

1.94

4b

OH

I

H

H

7.670

30.700

0.250

0.697

4c

OH

H

I

H

33.700

39.140

0.861

1.049

4d

OH

Br

H

H

4.250

2.350

1.809

0.547

4e

OH

H

Br

H

7.110

49.300

0.144

0.437

4f

OH

Cl

H

Cl

0.725

4.290

0.169

1.019

Ketoprofen

 

0.031

0.158

0.196

 
  1. P-values for the experiments p < 0.05