Host toxicity of the new fluconacenes against RPE and MRC-5 human cell lines (expressed as IC50) and inhibition of colony formation in S. cerevisiae treated with increasing concentrations of the 1a–4a for 24 h at 30 °C; fluconazole was used as parent drug for comparative purposes; values are expressed in μM. The activity of compounds 1a–4a on S. cerevisiae was evaluated via a newly established colony formation assay39.
| Compound | MRC5 | RPE | S. cerevisiae |
|---|---|---|---|
| Fluconazole | >100 | >100 | 51.0 ± 3.7 |
| 1a | 94.6 ± 2.4 | >100 | 13.2 ± 3.0 |
| 2a | 32.2 ± 0.1 | 74.7 ± 5.2 | 3.02 ± 2.18 |
| 3a | 70.4 ± 17.9 | 51.2 ± 0.1 | 5.86 ± 0.41 |
| 4a | 59.4 ± 2.8 | 48.4 ± 2.9 | 9.62 ± 0.56 |