Table 5.
In vitro activity against T. brucei brucei, cytotoxicity on murine macrophages and selectivity index (SI) values of the 5-nitrofuryl thiosemicarbazone ligands and their Ru p-cymene derivatives
| Compound | Macrophages IC50/μM | T. brucei IC50/μM | SI (fold)a |
|---|---|---|---|
| [Ru2(p-cymene)2(L1)2]Cl2 | >100 | 2.9 | >35 |
| [Ru2(p-cymene)2(L2)2](PF6)2 | ND | 10.6 | ND |
| [Ru2(p-cymene)2(L3)2](PF6)2 | ND | 17.3 | ND |
| [Ru2(p-cymene)2(L4)2]Cl2 | 26 | 0.5 | 52 |
| L1 | 64 | 1.1 | 58 |
| L2 | ND | 11.0 | ND |
| L3 | ND | 17.3 | ND |
| L4 | ND | >100 μM | ND |
| [Ru(p-cymene)Cl2]2 | ND | >100 μM | ND |
a
SI: IC50 macrophages/IC50 T. brucei brucei. ND: not determined. Results are the means of three different experiments.