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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