Table 2.
In vitro antiplasmodial activity in P. falciparum cultures of amyloid pan-inhibitors and β-sheet intercalators
| Compound | Chemical family | IC50 in 3D7 strain (µM) ± SEM | IC50 in K1 strain (µM) ± SEM | Selectivity index in vitro1 |
|---|---|---|---|---|
| HUP5ANTRAa | Aminoquinoline | 0.78 ± 1.86 | N/D | 97.7 |
| HUP7ANTRAa | Aminoquinoline | 7.53 ± 0.84 | N/D | 3.9 |
| HUP10ANTRAa | Aminoquinoline | 8.73 ± 1.61 | N/D | 9.7 |
| HUP7TH | Aminoquinoline | 0.13 ± 0.01 | 0.47 ± 0.36b | 60.0 |
| HUP8TH | Aminoquinoline | 0.21 ± 0.01 | 0.39 ± 0.14b | 23.3 |
| HUP9TH | Aminoquinoline | 0.16 ± 0.02 | 0.35 ± 0.06b | 30.6 |
| HUPH10TH | Aminoquinoline | 0.18 ± 0.05 | 3.50 ± 2.29b | 18.9 |
| HUPNTH | Aminoquinoline | 0.31 ± 0.02 | 0.43 ± 0.22b | 11.0 |
| HUPNTCl | Aminoquinoline | 0.15 ± 0.01 | 0.52 ± 0.13b | 42.0 |
| DP128c | Aminoquinoline | 0.65 ± 0.14 | N/D | 75.4 |
| DONE3TCl | Aminoquinoline | 0.08 ± 0.03 | 0.36 ± 0.07c | 157.5 |
| YAT2150 | Bis(styrylpyridinium) salt | 0.09 ± 0.02 | N/D | 37.8 |
| ThT | Benzothiazolium salt | 1.57 ± 0.23 | N/D | N/D |
| Congo Red | Bis(naphthalenesulfonate) | > 15 | N/D | N/D |