Table 1.
A table showing the DC50, IC50 and thermal stabilization afforded by ligands used in the study.
| Ligand | Linker Lengtha | No. of triazoles | DC50(nM) | IC50(nM) | ΔTm (°C) |
|---|---|---|---|---|---|
| Neomycin | NA | NA | 1474 ± 79 | 0.2 | |
| DPA 101 | NA | NA | ND | ND | 1.0 |
| DPA 123 | 5 | 1 | 33 | 272 ± 8 | 5.6 |
| DPA 119 | 11 | 2 | 78 | 1285 ± 155 | 3.0 |
| DPA 120 | 12 | 2 | 83 | 337 ± 43 | 3.4 |
| DPA 121 | 13 | 2 | 140 | 507 ± 9 | 4.1 |
| DPA 118 | 13 | 2 | 180 | 379 ± 20 | 3.0 |
| DPA 122 | 15 | 2 | 81 | 949 ± 92 | 5.4 |
| DPA 113 | 17 | 3 | 184 | 411 ± 51 | 2.5 |
| DPA 115 | 20 | 3 | 150 | 851 ± 80 | 2.1 |
| DPA 116 | 21 | 3 | 200 | 1368 ± 50 | 3.8 |
| DPA 117 | 23 | 3 | 180 | 1380 ± 150 | 4.0 |
a
The linker length was assigned by counting the number of main chain atoms between the 5’”-carbon on ribose ring (ring III, see Figure 1) of neomycin and oxygen atom on the phenolic end of the benzimidazole.