Table 13.
Antiproliferative activity of cisplatin and platinum(IV) prodrugs 25 and 26 on HCT-116 (colorectal cancer), HepG-2 (hepatocellular carcinoma), PC-3 (prostate carcinoma), LO-2 (normal liver), EA.hy926 (umbilical vein endothelial cell), SGC7901 (gastric cancer), and SGC7901/CDDP (cisplatin-resistant gastric cancer) cell lines. Rf: ratio of IC50 value for a cisplatin-resistant cell line and IC50 value for a cisplatin-sensitive line (IC50 SGC7901/CDDP / IC50 SGC7901).
| Compound/Cell Line | IC50, µM | |||||||
|---|---|---|---|---|---|---|---|---|
| HCT-116 | HepG-2 | PC-3 | LO-2 | EA.hy926 | SGC7901 | SGC7901/CDDP | Rf | |
| Cisplatin | 7.78 ± 0.63 | 3.96 ± 0.28 | 0.95 ± 0.07 | 3.54 ± 0.26 | 7.42 ± 0.36 | 1.11 ± 0.09 | 8.18 ± 0.73 | 7.37 |
| 25 | 4.94 ± 0.37 | 2.35 ± 0.18 | 0.81 ± 0.07 | 4.79 ± 0.32 | 9.61 ± 0.23 | 1.36 ± 0.09 | 4.50 ± 0.41 | 3.31 |
| 26 | 19.27 ± 1.4 | 9.67 ± 0.84 | 7.24 ± 0.26 | 59.64 ± 2.32 | 41.73 ± 2.1 | 3.27 ± 0.26 | 0.91 ± 0.06 | 0.29 |