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. 2014 Jun 5;57(12):5190–5202. doi: 10.1021/jm5001908

Table 2. Antiviral Potencies of Carboxamides 5a–5e in Cells Infected with HIV-1 Constructs Containing WT or Mutant IN.

      EC50 (FC, IN mutantsc)
  
compd CC50 (μM)a EC50 (nM, WT)b Y143R N155H G140S/Q148H SId
5a >250 372 ± 63 1× N/Ae N/Ae >672
5b >250 171 ± 57 3× N/Ae N/Ae >1462
5c >250 123 ± 21 3× N/Ae N/Ae >2033
5d >250 6.3 ± 2.4 16× 67× N/Ae >39683
5e >250 14 ± 1.9 2× 8× 32× >17857
a

Cytotoxic concentration resulting in 50% reduction in the level of ATP in human osteosarcoma (HOS) cells.

b

Values obtained from cells infected with lentiviral vector harboring WT IN.

c

Cells were infected with viral constructs carrying IN mutations and indicated values correspond to the fold-change (FC) in EC50 relative to WT.

d

Selectivity index calculated as the ratio of CC50 to EC50.

e

Not available.