Table 1 In vitro inhibitory activities and human plasma stability of GK470 analogs

From: Next generation thiazolyl ketone inhibitors of cytosolic phospholipase A2 α for targeted cancer therapy

 

cPLA2α

GVIA iPLA2

GV sPLA2

Stability in human plasma

 

% Inhib

XI(50)

% Inhib

% Inhib

4 h

20+ h

GK470

>90

0.011 ± 0.005

86

41

60.6

10.5.5¤

GK401

89

 

40

46

69.3

16.25¤

GK420

98

0.0016 ± 0.0002

0

46

63.3

18.05

GK419

50

 

0

29

82

52.7

GK427

98

0.0010 ± 0.0001

7.5

44

61.3

8.05

GK403

95

0.0014 ± 0.0001

34

32

21.5

ND¤

GK440

100

0.0010 ± 0.0001

0

31

21.3

0.9*

GK402

79

 

61

50

79.7

47.3¤

GK439

97

0.0029 ± 0.0004

67

53

59.9

12.8*

GK428

94

0.0038 ± 0.0001

54

36

35.9

1.65

GK449

98

0.0017 ± 0.0005

67

53

63

18.35*

  1. The % inhibition of each enzyme is reported at 0.091 mole fraction (% Inhib). XI(50)± stdev is reported for compounds showing >90% inhibition. The stability of the compounds in human plasma is reported as the % of the compound remaining after 4 h (4 h), and either 20 h, 24 h 39 min*, or 25 h ¤ (20+ h) incubation.
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