Table 1.
Anti-proliferative effects and ClogP values of TOA-amino acid derivatives.
| Compound | IC50 Values (μM) | ClogP | ||||
|---|---|---|---|---|---|---|
| HepG2 | HT-29 | Hela | BGC-823 | MDCK | ||
| CDDP | 2.856 | 6.112 | 9.838 | 6.819 | 3.691 | -b |
| TOA | 21.45 | -a | 8.683 | - | - | 8.125 |
| 6a | 1.999 | 2.498 | 3.256 | 3.062 | 4.884 | 7.433 |
| 6b | 2.322 | 4.770 | 7.690 | 4.474 | 5.125 | 7.835 |
| 6c | 2.391 | 3.213 | 6.754 | 4.976 | 5.034 | 8.590 |
| 6d | - | - | - | - | - | 8.763 |
| 6e | 5.969 | 9.830 | - | - | - | 8.750 |
| 6f | 4.257 | 5.956 | - | 9.522 | 9.785 | 8.479 |
| 6g | 2.270 | 2.347 | 2.383 | 2.481 | 2.310 | 7.343 |
| 6h | 8.216 | 9.503 | - | - | 8.119 | 8.831 |
| 6i | 10.22 | 16.85 | 12.61 | 16.04 | 15.78 | 8.346 |
| 6j | 5.785 | 5.480 | 11.47 | 10.73 | 12.62 | 8.117 |
| 6k | 11.44 | - | - | 10.01 | 10.82 | 8.895 |
| 6l | 4.783 | 4.829 | 5.217 | 4.898 | 3.122 | 6.860 |
The derivatives were evaluated on human hepatoma cell lines (HepG2), human colorectal cancer cell lines (HT-29), women cervical cancer cell lines (Hela) and human gastric cancer cell lines (BGC-823) using MTT assay, as well as their toxicity evaluation was carried out on Madin-Darby canine kidney cell lines (MDCK). -a meant IC50 > 25 μM, the compounds’ effects were considered to be weaker than TOA and not evaluated. Data are derived from three independent experiments. -b means the ClogP value was not calculated, due to structural differences between CDDP and others.