Table 1.
IC50 values (μM) of polyamine-based naphthalimide conjugates 5a-5c, 7a-7b, and 11a-11b, the positive control amonafide, and cisplatin by MTT assays[d].
 | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| IC50 (μM) | |||||||||||
| R= | m= | n= | p= | Snu-368 | Snu-739 | MDA-MB-231 | MCF-7 | A549 | A549cisR | RF[a] | |
| 5a | Cyclohexyl | 2 | 1 | / | 2.94 ± 0.06 | 2.16 ± 0.10 | 1.19 ± 0.12 | 2.3 ± 0.18 | 2.17 ± 0.20 | 3.62 ± 0.15 | 1.67 |
| 5b | Cyclohexyl | 2 | 2 | / | 2.72 ± 0.25 | 3.89 ± 0.35 | 1.07 ± 0.10 | 1.25 ± 0.10 | 1.75 ± 0.15 | 2.27 ± 0.25 | 1.30 |
| 5c | Cyclopropyl | 2 | 1 | / | 1.09 ± 0.10 | 0.76 ± 0.05 | 1.33 ± 0.12 | 1.35 ± 0.15 | 1.92 ± 0.23 | 0.83 ± 0.08 | 0.43 |
| 7a | Cyclopropyl | 2 | 1 | / | >30 | 25.77 ± 2.90 | 26.91 ± 2.65 | 8.62 ± 0.85 | 13.98 ± 1.39 | 17.38 ± 1.68 | / |
| 7b | H | 2 | 2 | / | >30 | >30 | >30 | >30 | >30 | 17.30 ± 1.78 | / |
| 11a | / | 1 | 1 | 1 | >50 | 9.69 ± 0.98 | 25.96 ± 2.56 | 14.81 ± 1.45 | 28.3 ± 2.85 | 16.33 ± 1.69 | / |
| 11b | / | 1 | 2 | 1 | >30 | 23.17 ± 2.36 | >30 | 25.91 ± 2.56 | >30 | 15.81 ± 1.58 | / |
| Amonafide | 13.98 ± 1.78 | 12.98 ± 1.56 | 14.89 ± 1.75 | 5.89 ± 0.56 | 6.89 ± 0.68 | 10.98 ± 1.02 | 1.59 | ||||
| FI[b] | 12.83 | 17.08 | 11.20 | 4.36 | 3.59 | 13.23 | 3.70 | ||||
| Cisplatin | 16.37 ± 1.26 | 10.02 ± 1.23 | 15.98 ± 1.59 | 9.60 ± 0.60 | 11.00 ± 0.15 | 40.36 ± 4.36 | 3.67 | ||||
| FI[c] | 15.02 | 13.18 | 12.02 | 7.11 | 5.73 | 48.63 | 8.74 | ||||
[a]
The RF (resistance factor) is defined as the IC50 value in A549cisR cells/IC50 value in A549 cells.
[b]
FI (fold increase) is defined as IC50(amonafide)/IC50(5c).
[c]
FI (fold increase) is defined as IC50(cisplatin)/IC50(5c).
[d]
An average of three measurements. ND = not determined.