Table 1.
In vitro trypanocidal activity of diamidines against T. b. brucei s427 and derivative cell lines (n = 3)a
| Compound | IC50 [nM] (SD) for s427 | IC50 [nM] (SD) for TbAT1−/− | RF | IC50 [nM] (SD) for B48 | RF |
|---|---|---|---|---|---|
| Pentamidine | 0.08 (± 0.01) | 0.35 (± 0.02) | 4 | 299 (± 17.0) | 3,738 |
| Diminazene | 13 (± 1.28) | 77 (± 13.1) | 6 | 43 (± 2.58) | 3 |
| DB75 | 1.5 (± 0.24) | 37 (± 7.23) | 25 | 32 (± 2.92) | 21 |
| DB820 | 15 (± 0.33) | 156 (± 9.38) | 10 | 86 (± 2.41) | 6 |
| CPD0801 | 136 (± 6.00) | 609 (± 103) | 4 | 380 (± 22.9) | 3 |
a
RF, resistance factor (i.e., the ratio of the IC50 value for a given compound for the derived cell line to its IC50 value for wild-type s427); S.D., standard deviation.