TABLE 6.
Toxicities and antileishmanial activities of tetrameric complexes of the C seriesa
| Compound | R1 | Log P | Log S | Pa | Toxicity (IC50, μM) | Antileishmanial activity (IC50, μM)
|
||
|---|---|---|---|---|---|---|---|---|
| Promastigotes | Amastigotes | SI | ||||||
| C19 | NH2 | 7.96 | −9.22 | <0.3 | 95.4 | 2.4 | 1.6 | 59.6 |
| C20 | NH2 | 8.42 | −9.16 | <0.3 | 69.7 | 0.9 | 0.5 | 139.4 |
| C14 | NH2 | 8.24 | −9.19 | <0.3 | 70.6 | 9.4 | 7.4 | 9.5 |
| C15 | NH2 | 8.45 | −9.12 | <0.3 | 45.9 | 0.9 | 0.6 | 76.5 |
| C17 | Cl | 9.95 | −10.63 | <0.3 | 65.1 | 68.4 | 51.4 | 1.2 |
| C18 | Cl | 9.75 | −10.69 | <0.3 | 66.6 | 65.1 | 30.2 | 2.2 |
| C9 | Cl | 10.05 | −10.59 | <0.3 | 64.2 | 66.4 | 44.1 | 1.4 |
| C10 | Cl | 9.85 | −10.65 | <0.3 | 65.8 | 68.1 | 28.8 | 2.3 |
a
Log P, lipophilicity; log S, solubility in water; Pa, predicted values for antileishmanial activity; SI, ratio between antileishmanial activity on amastigotes and toxicity.