Table 1.
Biological data for BABA derivatives and PTS1-BABA conjugates.[a]
| Entry | Compound | TbHK1% inhibition (10 μM) | TbHK1 IC50 (μM) | %BSF Growth Inhibition (10 μM) | BSF EC50 (μM) |
|---|---|---|---|---|---|
| 1 | 2 | – | 0.98 ± 0.067 | 6.9 ± 3.0 | >10 |
| 2 | 3 | 93.6 ± 2.8 | 3.5 ± 0.3 | 51.0 ± 14.3 | >10 |
| 3 | 11 | 0 | >10 | 9.6 ± 9.7 | >10 |
| 4 | 12 | 87.1 ± 3.5 | >10 | 24.5 ± 6.8 | >10 |
| 5 | 4 | 0 | >10 | 0 | >10 |
| 6 | 5 | 26.3 ± 3.8 | >10 | 0 | >10 |
| 7 | 6 | 10.5 ± 3.6 | >10 | 100 | 6.8 ± 1.5 |
| 8 | 7 | 67.5 ± 4.6 | 6.8 ± 0.2 | 38.9 ± 11.1 | >10 |
a
Trypanosome cultures were assayed in triplicate in a total volume of 40 μL, and the DMSO vehicle was used as a negative control. Percent inhibition was calculated by comparison to the growth of parasites grown with the DMSO controls from each plate. SID 17387000[2] was included in each assay as a positive control. Dose-response curves performed in triplicate for compounds that elicited > 50% growth inhibition at 10 μM were pursued in a 384-well plate format, with 50% effective concentrations (i.e. EC50) determined using GraphPad Prism (version 6.0) software (GraphPad Software, Inc., La Jolla, CA).