Table 8.
Antiproliferative activity of cisplatin-based prodrugs 1, 8 and 9 on A549 (lung carcinoma), HT-29 (colon cancer), HCT 116 (colon adenocarcinoma), SW480 (colorectal cancer), A2780 (ovarian cancer), and MSTO-21 (malignant pleural mesothelioma) cell lines.
| Compound/Cell Line | IC50, µM | ||||||
|---|---|---|---|---|---|---|---|
| A549 | HT-29 | HCT 116 | MSTO-211H | SW480 | A2780 | ||
| Log k’ | COX Expression | ||||||
| ++ | ++ | + | - | - | - | ||
| Cisplatin | −0.5 | 3.60 ± 0.90 | 2.72 ± 0.39 | 3.05 ± 0.28 | 1.33 ± 0.35 | 2.27 ± 0.12 | 0.46 ± 0.11 |
| Oxaliplatin | −0.28 | 0.74 ± 0.25 | 0.92 ± 0.08 | 1.16 ± 0.09 | 1.01 ± 0.55 | 0.48 ± 0.02 | 0.171 ± 0.008 |
| 1 | −0.32 | 6.40 ± 2.7 | 4.42 ± 0.21 | 1.50 ± 0.083 | 1.74 ± 0.21 | 0.217 ± 0.07 | 0.552 ± 0.123 |
| 8 | 0.14 | 0.825 ± 0.388 | 0.486 ± 0.235 | 0.184 ± 0.088 | 0.198 ± 0.035 | 0.0948 ± 0.023 | 0.063 ± 0.033 |
| 9 | 0.18 | 0.486 ± 0.075 | 0.313 ± 0.186 | 0.149 ± 0.076 | 0.161 ± 0.040 | 0.0844 ± 0.0287 | 0.045 ± 0.016 |