Table 9.
Antiproliferative activity of cisplatin-, carboplatin-, oxaliplatin-based and platinum(IV) prodrugs 16–20 on A549, A549R (cisplatin-sensitive and cisplatin-resistant lung carcinoma, respectively), SKOV-3 (ovarian cancer), CT-26 (colon cancer), and LO-2 (human normal liver) cell lines. Selectivity index (SI) = IC50(LO-2)/average IC50 values.
| Compound/Cell Line | IC50, µM | |||||
|---|---|---|---|---|---|---|
| A549 | A549R | SKOV-3 | CT-26 | LO-2 | SIa | |
| Cisplatin | 4.8 ± 0.6 | 15.1 ± 1.1 | 2.5 ± 0.4 | 0.3 ± 0.1 | 3.0 ± 0.7 | 0.5 |
| Oxaliplatin | 8.4 ± 2.2 | 7.3 ± 1.7 | 9.4 ± 2.3 | 2.30 ± 0.3 | 3.6 ± 0.5 | 0.5 |
| Carboplatin | 79.6 ± 18.4 | 60.6 ± 14.7 | 38.1 ± 9.6 | 46.2 ± 11.4 | 70.7 ± 16.3 | - |
| 16 | 2.2 ± 0.3 | 19.7 ± 2.5 | 14.4 ± 0.7 | 0.2 ± 0.1 | 1.9 ± 0.4 | 0.2 |
| 17 | 5.2 ± 0.5 | 4.8 ± 0.3 | 8.5 ± 0.1.6 | 2.9 ± 0.7 | 4.8 ± 0.8 | 0.9 |
| 18 | 47.2 ± 6.9 | 62.2 ± 16.7 | 26.0 ± 5.5 | 26.1 ± 8.6 | 39.9 ± 9.8 | 1.5 |
| 19 | 10.2 ± 1.0 | 12.0 ± 0.4 | 11.3 ± 0.8 | 8.2 ± 0.6 | 15.3 ± 2.5 | 0.5 |
| 20 | 27.3 ± 5.7 | 83.0 ± 16.4 | 48.9 ± 7.5 | 48.9 ± 8.4 | 26.3 ± 4.7 | 0.8 |