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Cellular uptake, DNA platination, and the ability of prodrugs 27–32 to inhibit HDAC and COX-2 and cause mitochondria depolarization in PSN-1 (pancreas cancer) cells.
| Class | Compound | Cellular Uptake, ng Pt/106 Cells | DNA platination, ng Pt/µg DNA | HDAC Inhibition, % | COX-2 Inhibition, % | Cells with Depleted Mitochondrial Potential, % |
|---|---|---|---|---|---|---|
| PDKi, COXi | 27 | 5 | 0.3 | <1 | 9 | 15 |
| 28 | 20 | 1.5 | <1 | 9 | 28 | |
| HDACi, COXi | 29 | 13 | 0.8 | 8 | 6.1 | 39 |
| 30 | 6 | 2.3 | 9 | 7.9 | 29 | |
| 31 | 17 | 0.75 | 7.5 | 11.2 | 32 | |
| 32 | 7.5 | 0.2 | 8 | 4.1 | 25 | |
| Cisplatin | 3 | 1.2 | 1 | 3 | 3 |
