Table 4.
Structures and EC50 Values for MMV676477 Structural Analogsa
| Compound ID | Structure | Amastigote EC50 ± SE (nM) |
Promastigote EC50 ± SE (nM) |
RAW 264.7 cells CC50 ± SE (nM) |
|---|---|---|---|---|
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| R = | ||||
| MMV676477 | 2-SCH3 | 79 ± 8.4 | 2400 ± 35 | 2200 ± 410 |
| SW100 | H | 1100 ± 84 | 2000 ± 130 | 690 ± 140 |
| SW22 | 160 ± 3.2 | 6700 ± 53 | 1300 ± 42 | |
| SW72 | 4-OCH3 | 180 ± 8.2 | 7500 ± 880 | > 10,000 |
| SW41 | 3-CI, 4-F | 20 ± 0.9 | 780 ± 29 | 2400 ±100 |
| SW73 | 2-CF3 | 68 ± 3.9 | 3200 ± 87 | 1500 ± 140 |
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||||
| R = | ||||
| SW75 | H | 290 ± 22 | 11200 ± 260 | 9900 ± 2800 |
| SW23 | −C(O)CH3 | > 3000 | > 50,000 | > 10,000 |
| SW101 | −C(O)NH-(4-CH3-C6H4) | 1100 ± 91 | 8200 ± 1600 | 3000 ± 250 |
| SW102 | −C(O)NH-(4-OCH3-C6H4) | 2400 ± 160 | 13000 ± 1400 | 5200 ± 380 |
| SW74 | −C(O)-(3-pyridyl) | 250 ± 40 | 9200 ± 1300 | 4200 ± 520 |
| SW10 | ![]() |
> 5000 | > 50,000 | > 10,000 |
and values for structural analogs of MMV676477 against L. amazonensis axenic amastigotes and promastigotes and the Mϕ cell line RAW 264.7 are shown. Shown are mean or values (nM) calculated from three biological replicates ± SE. Structure of each compound is provided. See Supplemental Methods for synthesis of these analogs.


