Table 4.
Compound | IC50 (μM)a | GI50 (μM)a | GI50 (μM)a | |
---|---|---|---|---|
C3H10T1/2b | ASZc | HUVEC | MERPMBc | |
| ||||
12 | 0.091 ± 0.02 | 0.077 ± 0.01 | 3.32 ± 0.55 | 2.0 ± 1.3 |
13 | 0.85 ± 0.1 | 0.071 ± 0.02 | 3.69 ± 1.1 | 2.9 ± 1.9 |
14 | 1.1 ± 0.17 | 2.5 ± 0.7 | 7.7 ± 4.4 | ND |
15 | >10 | 0.55 ± 0.07 | 78.3 ± 17.3 | ND |
16 | 0.47 ± 0.001 | 0.38 ± 0.07 | 18.3 ± 11.8 | ND |
17 | 1.85 ± 0.09 | 0.15 ± 0.038 | 2.5 ± 0.7 | 0.39 ± 0.2 |
18 | 0.54 ± 0.24 | 0.13 ± 0.04 | 12.1 ± 4.7 | ND |
19 | 6.6 ± 0.3 | 2.8 ± 0.9 | 65.0 ± 11.5 | ND |
20 | 0.19 ± 0.04 | 0.022 ± 0.01 | 53.2 ± 25.2 | 0.6 ± 0.2 |
21 | 2.4 ± 0.6 | 0.024 ± 0.02 | 12.8 ± 2.9 | 1.0 ± 0.5 |
22 | 4.1 ± 1.5 | 1.3 ± 0.65 | 26.5 ± 3.5 | ND |
23 | >10 | 1.4 ± 0.5 | 49.9 ± 15.9 | ND |
24 | >10 | 0.2 ± 0.08 | 84.1 ± 33.5 | 22.4 ± 12 |
25 | >10 | 0.54 ± 0.06 | 24.9 ± 2.2 | ND |
PSZ | 0.14 ± 0.02 | 0.54 ± 0.05 | 1.6 ± 0.02 | 1.5 ± 0.3 |
IC50 and GI50 values represent the Mean ± SEM of at least two separate experiments performed in triplicate.
All analogues evaluated following 24 hr incubation.
All analogues evaluated following 48 hr incubation.