Table 2.
Cell line | IC50 (μmol/L) |
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R1 = 5-Cl |
R1 = 5-Br |
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4d | Ent-4d | 4d′ | Ent-4d′ | 4g | Ent-4g | 4g′ | Ent-4g′ | |
MDM2 | 0.52 ± 0.07 | 0.13 ± 0.04 | 1.8 ± 0.12 | 1.5 ± 0.20 | 0.28 ± 0.06 | 0.08 ± 0.02 | 2.5 ± 0.3 | 1.3 ± 0.4 |
CDK4 | 0.78 ± 0.11 | 0.49 ± 0.13 | 3.9 ± 0.42 | 2.6 ± 0.37 | 0.32 ± 0.05 | 0.25 ± 0.08 | 10.6 ± 0.9 | 3.7 ± 0.6 |
U87MG | 8.3 ± 1.5 | 6.1 ± 1.3 | 60.4 ± 4.8 | 41.6 ± 3.9 | 4.9 ± 0.5 | 3.6 ± 0.7 | >50 | 28.6 ± 2.5 |
U251 | 17.8 ± 3.2 | 12.6 ± 2.3 | >50 | >50 | 8.6 ± 0.8 | 5.8 ± 1.1 | >50 | >50 |
Each compound was tested in triplicate; data are mean ± SD (n = 3). The IC50 value of anti-proliferation assays was obtained after 24-h incubation.