Table 1.
The cytotoxicity Topo I and II inhibitory activities of the target compounds.
| IC50 Values (μM) | Topo I Inhibition (%) | Topo II Inhibition (%) | |||||
|---|---|---|---|---|---|---|---|
| SMMC-7721 | HepG2 | LO2 | 100 μM | 20 μM | 100 μM | 20 μM | |
| 4a | 3.50 ± 0.61 | 3.31 ± 0.35 | 29.59 ± 2.12 | 15.1 | 5.6 | 69.7 | 25.9 |
| 4b | 4.42 ± 0.71 | 4.11 ± 0.55 | 31.06 ± 2.63 | 3.7 | -1 | 68.0 | 36.9 |
| 4c | 2.10 ± 0.21 | 2.24 ± 0.32 | 26.39 ± 1.32 | 0 | - | 68.7 | 38.3 |
| 4d | 1.75 ± 0.11 | 1.47 ± 0.12 | 16.03 ± 1.07 | 13.0 | 0 | 71.7 | 32.7 |
| 4e | 7.82 ± 0.78 | 10.72 ± 2.09 | >50 | 0 | - | 63.3 | 26.8 |
| 4f | 1.24 ± 0.16 | 1.35 ± 0.17 | 18.27 ± 0.78 | 0 | - | 73.7 | 31.3 |
| 5a | 2.02 ± 0.21 | 2.45 ± 0.38 | 21.32 ± 1.59 | 24.5 | 12.4 | 72.3 | 31.2 |
| 5b | 1.08 ± 0.22 | 1.26 ± 0.17 | 20.65 ± 1.73 | 34.2 | 9.0 | 72.5 | 38.2 |
| 5c | 1.15 ± 0.14 | 1.20 ± 0.24 | 15.85 ± 1.06 | 0 | - | 75.8 | 38.9 |
| 5d | 0.89 ± 0.11 | 1.04 ± 0.09 | 12.82 ± 0.83 | 0 | - | 81.1 | 41.3 |
| 5e | 3.75 ± 0.37 | 5.27 ± 0.67 | 28.62 ± 0.76 | 0 | - | 70.8 | 31.5 |
| 5f | 0.56 ± 0.08 | 0.91 ± 0.13 | 10.58 ± 0.52 | 0 | - | 83.5 | 43.2 |
| 6a | 1.21 ± 0.19 | 1.32 ± 0.21 | 15.23 ± 1.15 | 28.8 | 13.7 | 71.1 | 27.0 |
| 6b | 2.43 ± 0.21 | 2.91 ± 0.18 | 18.19 ± 1.64 | 15.1 | 0 | 69.0 | 31.7 |
| 6c | 3.62 ± 0.23 | 3.45 ± 0.25 | 28.42 ± 2.98 | 16.8 | 0 | 70.0 | 35.2 |
| 6d | 2.72 ± 0.31 | 2.31 ± 0.21 | 18.65 ± 1.36 | 0 | - | 72.5 | 32.8 |
| 6e | 4.55 ± 1.56 | 7.84 ± 2.31 | 35.39 ± 3.13 | 0 | - | 65.6 | 28.2 |
| 6f | 0.65 ± 0.07 | 1.01 ± 0.12 | 13.72 ± 1.28 | 0 | - | 81.8 | 39.8 |
| 7a | >50 | >50 | >50 | 0 | - | 23.8 | 9.7 |
| 7b | >50 | >50 | >50 | 2.0 | - | 17.8 | 9.8 |
| 7c | >50 | >50 | >50 | 0 | - | 16.9 | 8.1 |
| CPT 2 | 0.56 ± 0.18 | 1.12 ± 0.26 | 8.93 ± 0.52 | 75.1 | 38.2 | - | - |
| VP-16 | 0.36 ± 0.10 | 0.57 ± 0.16 | 5.92 ± 0.29 | - | - | 88.5 | 47.8 |
| DOX | 0.68 ± 0.11 | 0.81 ± 0.19 | 5.32 ± 0.67 | - | - | - | - |
1 -: Not tested. 2 CPT: camptothecin; VP-16: etoposide; DOX: doxorubicin.