Table 1.
Activity profiles of inhibitors 4–11a
Compd | ||||||
---|---|---|---|---|---|---|
Structure | Compound code names | IC50 (μM) PfDHODH | EC50 (μM) Pf3D7 | IC50 (μM) hDHODH | IC50 (μM) PbDHODH | |
1* |
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DSM1 | 0.047 | 0.076 | > 100 | 0.23 |
2* |
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DSM74 | 0.28 | 0.34 | > 100 | 0.38 |
4 |
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DSM154 | > 100 | >100 | > 100 | > 100 |
5 |
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DSM155 | > 100 | > 50 | > 100 | > 100 |
6 |
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DSM71 | 0.15±0.01 | 0.19 (0.15 – 0.25) | > 100 | 2.8±0.28 |
7 |
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DSM96 | 4.8±0.7 | 5.2 (3.6 – 6.7) | n.d. | 6.3±0.80 |
8 |
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DSM68 | 0.4±0.09 | 0.91 (0.80 – 1.0) | > 100 | 3.3±0.4 |
9 |
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DSM23 | 0.44±0.17 | 2.2 (1.2 – 3.7) | > 100 | 11±3.3 |
10 |
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DSM70 | > 100 | > 12.5 | n.d. | n.d. |
11 |
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DSM105 | > 50 | > 5 | n.d. | >50 |
12 |
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DSM25 | 4.8±0.38 | 3.2 (2.4 – 3.5) | n.d. | > 10 |
13 |
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DSM78 | 27±6.3 | > 10 | n.d. | n.d. |
14 |
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DSM79 | >25 | 3.2 (2.4 – 4.3) | n.d. | n.d. |
15 |
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DSM80 | > 100 | > 25 | n.d. | n.d. |
16 |
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DSM151 | 0.077 ± 0.008 | 0.32 (0.30 – 0.35) | > 100 | 0.17 ± 0.018 |