TABLE 4.
Activity of spiro-β-lactams against HIV-1.
Compound | CC50 μM | MPI (%) 25 μg/mL | IC50 HIV-1 μM | IC90 HIV-1 μM | Therapeutic index (CC50/IC50) |
---|---|---|---|---|---|
BSS-730A | 76.84 | 99 | 0.014 | 0.025 | 5488.57 |
9a | 215.46 | 0 | Nd | Nd | Nd |
9b | 54.67 | 0 | Nd | Nd | Nd |
9c | 58.13 | 0 | Nd | Nd | Nd |
9d | 38.02 | 54 | Nd | Nd | Nd |
9e | 60.29 | 44 | Nd | Nd | Nd |
9f | 53.40 | 21 | Nd | Nd | Nd |
9g | 45.28 | 0 | Nd | Nd | Nd |
9h | 55.99 | 0 | Nd | Nd | Nd |
9i | 35.78 | 100 | 0.015 | 0.020 | 2385.33 |
9j | 60.03 | 93 | 0.089 | 0.209 | 674.49 |
9k | 54.06 | 84 | 0.366 | Nd | 148.11 |
9l | 55.83 | 100 | 0.111 | 0.221 | 502.97 |
9m | 60.11 | 94 | 0.203 | 0.437 | 296.11 |
9n | 62.29 | 100 | 0.017 | 0.046 | 3664.12 |
9o | 44.74 | 0 | Nd | Nd | Nd |
12a | 58.14 | 93 | 0.019 | 0.054 | 3060.00 |
12b | 55.99 | 92 | 0.063 | 0.104 | 888.73 |
12c | 55.02 | 87 | 0.050 | 0.116 | 1100.40 |
12d | 53.00 | 80 | 0.178 | 0.413 | 297.75 |
12e | 64.40 | 76 | 1.304 | 1.504 | 49.39 |
12f | 70.14 | 88 | 0.132 | 0.585 | 531.34 |
12h | 73.63 | 0 | Nd | Nd | Nd |
12i | 78.30 | 87 | 0.140 | 0.223 | 559.29 |
13a | 64.77 | 0 | Nd | Nd | Nd |
13b | 63.68 | 0 | Nd | Nd | Nd |
13c | 50.65 | 0 | Nd | Nd | Nd |
13d | 73.79 | 0 | Nd | Nd | Nd |
13e | 54.74 | 0 | Nd | Nd | Nd |
13f | 58.75 | 0 | Nd | Nd | Nd |
13h | 56.17 | 0 | Nd | Nd | Nd |
13i | 61.21 | 0 | Nd | Nd | Nd |
14a | 75.06 | 100 | 0.012 | 0.048 | 6255.00 |
14b | 78.26 | 95 | 0.146 | 0.338 | 494.93 |
14c | 77.61 | 100 | 0.015 | 0.018 | 5174.00 |
14d | 133.60 | 100 | 0.015 | 0.019 | 8906.67 |
14e | 100.10 | 94 | 0.211 | 0.720 | 474.41 |
14f | 87.48 | 97 | 0.067 | 0.198 | 1305.67 |
14g | 100.60 | 100 | 0.030 | 0.099 | 3353.33 |
14h | 72.12 | 93 | 0.111 | 0.297 | 649.73 |
14i | 66.87 | 95 | 0.143 | 0.305 | 467.62 |