TABLE 1.
Complex | IC50 (nM) for T. gondii beta-gal | IC50 (μM) for HFFs | LogP for RSH group |
---|---|---|---|
1 | 34 ± 4 | 800 | 2.98 ± 0.28 |
2 | 62 ± 10 | >1,000 | 4.21 ± 0.29 |
3 | 540 ± 60 | ND | 2.38 ± 0.32 |
4 | 130 ± 20 | ND | 2.83 ± 0.42 |
5 | 120 ± 20 | ND | 1.68 ± 0.29 |
9 | 1.2 ± 0.5 | 5,129 | ND |
Chloride salts of the corresponding thiols of complexes 1 to 5 and 9 were used for all experiments. For the determination of efficacies, confluent HFF monolayers grown in a 96-well plate were treated with the complexes at various concentrations and were infected with T. gondii beta-gal tachyzoites (103 per well). After 3 days, beta-galactosidase activity or host cell viability was determined, and IC50s were calculated as described in the text. The logP values correspond to the values that were calculated for the thiol RSH groups (17). ND, not done.