Table 1.
Anti-proliferative effects and ClogP values of the target compounds and starting materials.
| Compound | IC50 (μM) | ClogP | |||||
|---|---|---|---|---|---|---|---|
| Bel-7402 | HT-29 | HepG2 | MCF-7 | Hela | MDCK | ||
| TMP, OA, UA, GA, BA | >20 a | >20 | >20 | >20 | >20 | ND b | NC c |
| 1a | 10.24 | 13.22 | 14.85 | 15.17 | 14.07 | >20 | 9.72 |
| 1b | >20 | >20 | 12.09 | 10.55 | >20 | >20 | 11.26 |
| 1c | >20 | >20 | >20 | >20 | >20 | ND | 12.32 |
| 1d | 9.28 | 8.43 | 7.94 | 5.69 | 4.37 | 16.39 | 10.16 |
| 2a | 8.01 | 17.61 | >20 | >20 | 19.96 | >20 | 9.72 |
| 2b | >20 | >20 | >20 | >20 | >20 | ND | 11.26 |
| 2c | >20 | >20 | >20 | >20 | >20 | ND | 12.32 |
| 2d | 10.14 | 9.70 | >20 | 9.49 | 9.66 | >20 | 10.16 |
| 3a | >20 | 19.87 | >20 | >20 | 11.17 | >20 | 7.57 |
| 3b | >20 | >20 | >20 | >20 | >20 | >20 | 9.08 |
| 3c | >20 | >20 | 9.06 | 7.58 | 17.51 | >20 | 10.14 |
| 3d | >20 | >20 | >20 | >20 | >20 | ND | 7.99 |
| 4a | 4.19 | 5.23 | 4.48 | 4.23 | 4.34 | >20 | 9.57 |
| 4b | >20 | >20 | 13.20 | 12.87 | >20 | >20 | 11.11 |
| 4c | >20 | >20 | >20 | >20 | >20 | ND | 12.17 |
| 4d | 13.35 | 8.38 | 7.42 | 6.22 | 12.15 | >20 | 10.01 |
| DDP | 5.91 | 5.28 | 4.57 | 5.17 | 6.22 | 14.61 | NC |
a IC50 > 20.0 μM. We set a strict standard to the evaluation of antiproliferative activities. The maximal concentration of tested compounds is 20.0 μM. When IC50 > 20.0 μM, we considered the antiproliferative activities of the compounds were too weak to do further research; b “ND” not determined, due to the weak cytotoxicity, IC50 value of compounds on MDCK cells was not be detected; c “NC” means the ClogP value was not calculated.