Table 2. G4 Selectivity of the Selected Compoundsa.
| ΔT1/2 (°C)b |
|||
|---|---|---|---|
| Comp | F-c-kit1-T | F-c-kit1-T + hairpin (1:15) | F-ckit1-T + hairpin (1:50) |
| 1 | 25.4 (±0.5) | 22.2 (±0.5) | 19.2 (±0.5) |
| 2 | 22.4 (±0.5) | 21.4 (±0.5) | 20.2 (±0.5) |
| 8 | 24.6 (±0.5) | 21.4 (±0.5) | 19.6 (±0.5) |
| 10 | 26.6 (±0.5) | 24.8 (±0.5) | 23.8 (±0.5) |
| 15 | 22.0 (±1.0) | 21.6 (±1.0) | 22.2 (±1.0) |
| 19 | 8.0 (±0.4) | 7.8 (±0.4) | 8.4 (±0.4) |
| 20 | 10.0 (±0.4) | 11.1 (±0.5) | 12.1 (±0.5) |
a
G4/dsDNA competition determined by ligand-induced thermal stabilization of F-c-kit1-T G4 measured by FRET. ΔT1/2 values are the differences between the T1/2 of F-c-kit1-T in the presence (2 molar equiv) and absence of the ligands, without or with large excess of unlabeled hairpin (15 and 50 molar equiv with respect to G4).
b
The T1/2 of F-ckit1-T is 57.4 (±0.2) °C. All experiments were performed at least in duplicate, and the reported values are the average of the measurements. The differences between results of CD and FRET melting experiments could be explained with different DNA sequences and/or experimental conditions.