Table 8. In vitro cytotoxicity of the selected iridium(iii) porphyrin complexes against a panel of human cancer cell lines a b c .
| IC50 (μM)
b
|
IC50 (μM) |
PI c | Uptake d | Log P e | ||||||
| HeLa | HepG2 | MCF-7 | HCT116 | HCC827 | NCI-H460 (dark) | NCI-H460 (light) | ||||
| 1d′ | 0.37 ± 0.10 | 1.60 ± 0.21 | 0.71 ± 0.04 | 0.42 ± 0.06 | 0.55 ± 0.11 | 0.46 ± 0.10 | 0.04 ± 0.003 | 11.5 | 235.9 ± 9.81 | 2.67 |
| 2a | 0.17 ± 0.1 | 2.1 ± 0.3 | 0.65 ± 0.2 | 0.14 ± 0.04 | 2.29 ± 0.50 | 1.22 ± 0.03 | 0.11 ± 0.08 | 11.1 | 147.6 ± 6.4 | 3.03 |
| 2c | 0.03 ± 0.01 | 0.93 ± 0.1 | 0.16 ± 0.1 | 0.14 ± 0.1 | 1.1 ± 0.3 | 0.15 ± 0.05 | 0.009 ± 0.004 | 16.7 | 309.7 ± 46.7 | 2.96 |
| 2e | 0.10 ± 0.1 | 2.4 ± 0.2 | 0.73 ± 0.5 | 0.11 ± 0.03. | 0.69 ± 0.01. | 0.16 ± 0.04 | 0.006 ± 0.002 | 26.7 | 158.7 ± 29.5 | 3.23 |
| 2f | 0.10 ± 0.1 | 0.94 ± 0.1 | 0.26 ± 0.1 | 0.4 ± 0.2 | 1.23 ± 0.10 | 0.31 ± 0.04 | 0.03 ± 0.002 | 10.3 | 131.3 ± 10.2 | 2.76 |
| 3 | 7.9 ± 0.5 | >100 | >100 | 23 ± 3.3 | 50 ± 3.6 | 2.9 ± 0.02 | 0.12 ± 0.02 | 24.2 | 116.2 ± 20.6 | 3.11 |
| 4 | 0.10 ± 0.01 | 1.32 ± 0.10 | 0.12 ± 0.02 | 0.25 ± 0.08 | 1.27 ± 0.32 | 0.11 ± 0.005 | 0.005 ± 0.001 | 23.1 | 305.1 ± 57.2 | 2.83 |
| [IrIII(oep)Cl(CO)] | >50 | >50 | >50 | >50 | >50 | >50 | 19.70 ± 1.0 | >2.5 | 34.1 ± 2.8 | 2.38 |
| Cisplatin | 3.80 ± 0.51 | 6.18 ± 0.82 | 13.20 ± 1.03 | 6.94 ± 0.54 | 9.61 ± 0.81 | 3.96 ± 0.48 | 4.61 ± 0.31 | 0.86 | — | — |
aHeLa, cervical epithelial carcinoma; HepG2, hepatocellular carcinoma; MCF-7, breast carcinoma; HCT-116, colorectal carcinoma; HCC827, non-small cell lung carcinoma; NCI-H460, non-small cell lung carcinoma.
bIC50 values were examined by MTT assay after incubation of drugs for 72 h.
cPI = IC50(dark)/IC50(light).
dCellular uptake was determined by the iridium content (μg) in the cellular proteins (g) after treatment of the NCI-H460 cells with each complex (1 μM) for 2 h.
eLipophilicity was determined by measuring the ratio of the amount of iridium (μg) in each complex partitioned in n-octanol and saline solution (0.9%, w/v).