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Table 1 Antiviral activity and toxicity of selected hits in multiple round MTT assay

From: Inhibitors of the integrase–transportin-SR2 interaction block HIV nuclear import

Class

Compound ID

IN–TRN-SR2 Pin at 50 µM (%)a

EC50 (µM)b

CC50 (µM)c

Protection (%)d

3

MVG001

65.3

<

8

<

8

2

MVG002

43.4

>

13

=

13

5

MVG003

47.2

>

80

=

80

13

MVG004

82.6

>

21

=

21

4

MVG005

39.7

>

57

=

57

6

MVG006

50.5

>

63

=

63

6

MVG007

64.8

>

74

=

74

6

MVG008

30.1

>

99

=

99

23

MVG009

32.0

>

51

=

51

4

6

MVG010

37.1

>

100

=

100

6

MVG011

41.7

>

102

=

102

1

MVG012

107.1

>

74

=

74

10

MVG013

51.9

>

95

=

95

3

MVG014

63.8

>

87

=

87

4

MVG015

48.1

>

87

=

87

5

MVG016

46.9

>

244

>

244

20

MVG017

< 10

=

195

=

229

52

MVG018

< 10

>

137

>

137

7

MVG019

< 10

>

250

>

250

6

MVG020

< 10

>

250

>

250

18

MVG021

< 10

>

250

>

250

34

MVG022

44.9

=

67

>

136

53

MVG023

< 10

>

110

>

110

0

MVG024

< 10

>

36

>

45

49

7

MVG025

72.9

>

34

=

34

4

MVG026

45.7

>

35

=

48

4

MVG027

43.2

>

57

=

57

6

MVG028

58.7

>

56

=

80

13

MVG029

48.8

>

57

=

57

3

MVG030

71.6

>

97

=

97

25

MVG031

62.3

>

53

=

53

4

MVG032

46.5

>

48

=

48

5

MVG033

49.5

>

59

=

59

20

MVG034

43.0

>

73

=

73

16

9

MVG035

43.8

>

36

=

36

1

MVG036

105.6

>

55

=

65

46

MVG037

43.1

>

85

=

85

22

MVG038

47.2

>

59

=

59

0

MVG039

40.1

>

17

=

17

1

MVG040

43.6

>

25

=

25

25

MVG041

54.0

>

35

=

35

2

10

MVG042

89.6

>

55

=

55

10

MVG043

102.0

>

67

=

67

4

MVG044

75.9

>

250

>

250

22

MVG045

11.4

>

203

=

203

21

MVG046

10.3

>

207

=

207

32

MVG047

< 10

>

250

>

250

7

MVG048

< 10

>

87

=

87

0

MVG049

< 10

=

165

>

231

55

MVG050

44.1

>

250

>

250

0

MVG051

< 10

>

250

>

250

22

MVG052

20.1

>

66

=

66

8

MVG053

< 10

>

167

>

167

39

MVG054

18.0

>

225

=

225

0

MVG055

< 10

>

167

>

167

21

MVG056

71.1

>

250

>

250

24

MVG057

23.3

>

250

>

250

16

MVG058

53.7

=

170

>

250

24

  1. aCompounds were tested in AlphaScreen at 50 µM for their ability to inhibit the IN-TRN-SR2 interaction. Percentage inhibition (PIN), relative to the DMSO control
  2. b,cMT-4 cells were infected with HIV at 100 to 300× the 50% cell culture infective doses in the presence of 100 µM of the antiviral drugs. The compound concentration achieving 50% protection against the cytopathic effect of HIV, the 50% effective concentration (EC50), was determined. The concentration of the compound killing 50% of the MT-4 cells, the 50% cytotoxic concentration (CC50), was determined as well
  3. dThe percentage of protection against the cytopathic effect of HIV was measured in MT-4 cells as well. Values below 20% were not considered as real activities. Data are averages of triplicate measurements