Table 1.
In vitro drug sensitivity of 7-deazapurine nucleoside analogues.
| Cpd. | T. b. brucei EC50 (µM) | T. b. rhodesiense EC50 (µM) | MRC-5 EC50 (µM) | SI (MRC/T.b. brucei) | SI (MRC/T.b. rhodesiense) |
|---|---|---|---|---|---|
| Tubercidin, 6 | 0.48 ± 0.1 | 0.036 ± 0.001 | 2.2 ± 0.7 | 4 | 61 |
| 8 | 1.2 ± 0.3 | 0.12 ± 0.02 | 12 ± 2 | 10 | 107 |
| 9 | 0.048 ± 0.009 | 0.00052 ± 0.00004 | >64 | >1333 | >123,077 |
| 10 | 0.0013 ± 0.0003 | 0.00040 ± 0.00009 | 15 ± 3 | 11,462 | 37,500 |
| 11 | 48 ± 1 | >64 | >64 | 1.3 | – |
| 12 | 0.46 ± 0.08 | 0.12 ± 0.01 | 6.1 ± 0.7 | 13 | 50 |
EC50 values, determined with the Alamar blue cell viability assay, are expressed in µM, and represent mean and SEM. The number of independent replicates was n = 5 (8, 9, 10), n = 4 (6) and n = 2 (11 and 12). Cytotoxicity was assessed in human MRC-5 fibroblasts. Source data are provided as a Source Data file
SI selectivity index