Table 5. Antiviral Potencies of 5o–5q and 5v Compared with 1, 2, and Previously Reported Carboxamides 3 and 4(9) in Cells Infected with HIV-1 Constructs Containing WT or Mutant IN.
| EC50 [nM/(FC), IN mutantsb] |
||||||
|---|---|---|---|---|---|---|
| compd | EC50 (nM, WT)a | Y143R | N155H | R263 K | G118R | G140S/Q148H |
| 1 | 4 ± 2 | 162 ± 16 (41×) | 154 ± 33 (38×) | 9 ± 4 (2×) | 36 ± 5 (9×) | 1900 ± 300 (475×) |
| 2 | 1.6 ± 0.9 | 4.3 ± 1.2 (3×) | 3.6 ± 1.3 (2×) | 11 ± 3 (7×) | 13 ± 5 (8×) | 5.8 ± 0.5 (4×) |
| 3 | 5.1 ± 1.9 | 4.9 ± 0.8 (1×) | 134 ± 23 (26×) | N/Ac | N/Ac | 438 ± 121 (86×) |
| 4 | 6.2 ± 2.9 | 11 ± 2 (2×) | 31 ± 8 (5×) | 36 ± 8 (6×) | 107 ± 8 (17×) | 308 ± 125 (50×) |
| 5o | 5.2 ± 0.6 | 4.6 ± 1.8 (0.88×) | 25 ± 4 (5×) | 26 (5×) | 27 ± 1 (5×) | 43 ± 15 (8×) |
| 5p | 4.5 ± 1.5 | 4.8 ± 2.9 (1×) | 3.1 ± 0.3 (0.69×) | 16 ± 5 (4×) | 44 ± 11 (10×) | 35 ± 14 (8×) |
| 5q | 3.8 ± 1.2 | 4.6 ± 2.2 (1×) | 19 ± 7 (5×) | 26 ± 8 (7×) | 41 ± 18 (11×) | 36 ± 16 (9×) |
| 5v | 1.1 ± 0.66 | 2.5 ± 0.6 (2×) | 5.3 ± 2.3 (5×) | 6.4 ± 2.3 (6×) | 16 ± 5 (15×) | 35 ± 9 (32×) |
a
Values obtained from cells infected with lentiviral vector harboring WT IN.
b
Cells were infected with viral constructs carrying IN mutations and indicated values correspond to the fold-change (FC) in EC50 relative to WT.
c
Not available.