Table 4.
In vitro cytotoxicity (IC50 values in μM) of HQNO2-L-Pro and its RuCym and RhCp* complexes in Colo205, Colo320 {72 h exposure}, MES-SA and MES-SA/Dx5 {144 h exposure} cell lines. IC50 values obtained for the analogous HQCl-L-Pro compounds are also shown for comparison. IC50 values obtained for HQNO2-L-Pro in the presence of various equiv. CuCl2, ZnCl2 and FeCl3. Doxorubicin was used as a control.
| IC50 (μM) | ||||
|---|---|---|---|---|
| MES-SA | MES-SA/Dx5 | Colo205 | Colo320 | |
| ligand alone | ||||
| HQNO2-L-Pro | 226 ± 17 | 97 ± 29 | 34 ± 1 | 32.4 ± 0.4 |
| HQNO2-L-Pro + TQ | 223 ± 6 | 219 ± 46 | - | - |
| HQCl-L-Pro | 23 ± 4 | 4.3 ± 0.1 | 23 ± 3 a | 9 ± 2 a |
| complexes | ||||
| RuCym-HQNO2-L-Pro | 166 ± 37 | >400 | >100 | >100 |
| RhCp*-HQNO2-L-Pro | 167 ± 38 | 106 ± 8 | 35 ± 1 | 29.8 ± 0.2 |
| RuCym-HQCl-L-Pro | - | - | 68 ± 11 a | >100 a |
| RhCp*-HQCl-L-Pro | - | - | 26 ± 5 a | 10 ± 1 a |
| incubation of HQNO2-L-Pro with metal salts | ||||
| +1 equiv. Cu(II) | 40 ± 7 | 25 ± 6 | - | - |
| +0.5 equiv. Cu(II) | 49 ± 15 | 35 ± 11 | - | - |
| +1 equiv. Zn(II) | 164 ± 24 | >400 | - | - |
| +0.5 equiv. Zn(II) | >400 | >400 | - | - |
| +1 equiv. Fe(III) | 89 ± 9 | 47 ± 9 | - | - |
| +0.33 equiv. Fe(III) | 121 ± 27 | 53 ± 9 | - | - |
| doxorubicin | 0.03 ± 0.01 | 4 ± 1 | 0.71 ± 0.02 | 5.4 ± 0.9 |
a Data are taken from Ref. [12].