Table 1.
Median IC50 and interquartile range (IQR) of HDACi candidates against P. falciparum clinical isolates, and laboratory strains 3D7 and Dd2.
| Compound ID | Median IC50 (IQR) in nM | SI | |||||
|---|---|---|---|---|---|---|---|
| Clinical isolates – children & adults combineda | Clinical isolates – children onlya | Clinical isolates – adults onlya | 3D7b | 3D7c | Dd2c | ||
| 1a |
47.1 (15.9–386.9) |
42.6 (20.2–175) |
116 (11.7–910) |
21.3 | 20 ± 10 | 12 ± 8 | >1295 |
| 1d |
21.9 (8.8–97.8) |
21.6 (9.1–71.4) |
25.9 (7.1–127) |
8.7 | 11 ± 4 | 14 ± 6 | >850 |
| 1g |
167 (34.6–1022) |
117 (34.1–1268) |
326 (37.7–1020) |
49.4 | 25 ± 18 | 31 ± 12 | >1613 |
| 1h |
38.4 (11.0–96.3) |
26.3 (12.6–92.8) |
73.7 (10.0–97.3) |
23.3 | 9 ± 3 | 15 ± 6 | >520 |
| 1i |
174 (61.7–406) |
126 (71.0–413) |
215 (45.9–405) |
54.9 | 21 ± 16 | 33 ± 15 | >642 |
| 1u |
13.6 (4.4–89.8) |
14.7 (4.6–76.9) |
13.1 (3.1–146) |
12.1 | 4 ± 1 | 1 ± 1 | >2496 |
| 1v |
65.1 (28.7–220) |
54.3 (26.6–95.9) |
110 (38.9–316) |
9.8 | 14 ± 4 | 14 ± 4 | >499 |
| 2c |
410 (152–966) |
287 (168–861) |
619 (130–1116) |
150.4 | 95 ± 15 | ND | >526 |
| 2g |
47.8 (9.6–215) |
31.2 (9.6–231) |
113 (6.8–200) |
40.7 | 8.8 ± 3.2 | ND | 1483 |
| 2h |
26.9 (5.2–94.5) |
17.8 (5.6–93.3) |
35.6 (3.8–95.5) |
11.8 | 5.2 ± 3.6 | ND | 889 |
| 2i |
32.1 (17.7–59.1) |
28.0 (17.5–44.0) |
40.8 (21.9–71.0) |
11.3 | 9.7 ± 2.9 | ND | 64 |
| 2m |
348 (191–760) |
351 (193–834) |
337 (178–535) |
209.5 | 87 ± 44 | ND | 234 |
| SAHA |
267 (172–392) |
276 (166–395) |
267 (187–372) |
187.3 | 139 ± 73 | 146 ± 22 | >15 |