Table 1 In vitro inhibitory potency and selectivity of 2-oxoesters.

From: 2-Oxoesters: A Novel Class of Potent and Selective Inhibitors of Cytosolic Group IVA Phospholipase A2

Entry

No

Structure

GIVA cPLA2

GVIA iPLA2

GV sPLA2

ClogP

% Inhibitiona

X I(50)

% Inhibitiona

X I(50)

% Inhibitiona

1

10e

68.2 ± 2.7

 

69.4 ± 12.2

 

27.5 ± 0.9

6.51

2

12e

78.4 ± 3.5

 

<25

 

<25

5.63

3

17a

>95

0.00008 ± 0.00001

<25

 

<25

6.76

4

20

<25

 

<25

 

41.0 ± 0.2

6.82

5

17b

>95

0.00289 ± 0.00043

<25

 

52.6 ± 5.3

5.46

6

16c

<25

 

<25

 

<25

4.58

7

19

27.3 ± 4.8

 

<25

 

<25

3.87

8

17d

>95

0.00068 ± 0.00007

<25

 

<25

4.78

9

17e

 > 95

0.00007 ± 0.00001

25

 

<25

6.68

10

17f

 > 95

0.000078 ± 0.00001

65 ± 3.4

 

<25

4.70

11

17g

 > 95

0.0065 ± 0.002

84 ± 1.5

 

<25

4.25

12

17h

 > 95

0.0010 ± 0.0003

94 ± 1.4

 

<25

4.17

13

10a

<25

 

72 ± 4

 

<25

 

14

10b

55 ± 4.0

 

 > 95

0.0052 ± 0.0007

<25

3.81

15

4

>95

0.00008 ± 0.000005c

   

8.50

  1. a% Inhibition at 0.091 mole fraction of each inhibitor. bIC50 4.3 nM in a vesicle assay32.
Back to article page