TABLE 2.
In vitro activities of 1–6 and positive controls against T. brucei bloodstream forms and ovarian cancer cell lines.
| Compounds | Activity against T. brucei IC50, nM±SE (SI) a , b | Activity against T. brucei IC90, nM±SE a | Activity against A2780/WT cells, IC50, µM±SE | Activity against A2780/ADR cells, IC50, µM±SE | Activity against A2780/cis cells, IC50, µM±SE |
|---|---|---|---|---|---|
| 1 | 306 c | NT | 0.44 ± 0.2 | 1.27 ± 0.6 | 0.67 ± 0.39 |
| 2 | 16.7 ± 0.7 (309) | 39.7 ± 0.7 | NT | NT | NT |
| 3 | 199 ± 15 | 256 ± 6 | 0.07 ± 0.01 | 0.17 ± 0.04 | 0.23 ± 0.02 |
| 4 | 28.3 ± 0.5 (240) | 40.3 ± 6.1 | 0.20 ± 0.58 | 0.31 ± 0.06 | 0.58 ± 0.1 |
| 5 | 81.3 ± 2.5 (82.4) | 113 ± 11 | 0.06 ± 0.01 | 0.18 ± 0.01 | 0.31 ± 0.19 |
| 6 | 59 ± 13 (478) | 114 ± 11 | 0.13 ± 0.07 | 0.18 ± 0.02 | 0.28 ± 0.05 |
| Cisplatin | — | — | 3.47 ± 2.2 | NT | 24.67 ± 2.75 |
| Doxorubicin | — | — | 0.07 ± 0.06 | 3.03 ± 0.35 | NT |
a
Tested as hydrochloride salts except for 6, tested as citrate.
b
Selectivity index compared with cytotoxicity to Hep G cells (Table 1).
c
Data from Oluwafemi et al. 2009. Each datum represents the mean ± SE of at least three independent experiments.