Table 1.
DC50 and rbl or rdl values of (−)-lomaiviticin A (1) and duplexed DNA
Entry | Polynucleotide DNA | DC50 (per base pair) | rbl |
1 | dAdT | 235 ± 10 nM | 3.0 |
2 | dGdC | 770 ± 44 nM | 1.25 |
3 | dA•dT | 245 ± 15 nM | 2.1 |
Oligonucleotide duplexes | DC50 (per duplex) | rdl | |
4 | GCGC: d(CGCGCGCGCGCG)2 | 18.3 ± 1.4 μM | 0.09 |
5 | ATAT: d(CGCATATATGCG)2 | 1.87 ± 0.14 μM | 0.5 |
6 | Dickerson: d(CGCAAATTTGCG)2 | 2.14 ± 0.18 μM | 0.5 |
7 | A6T6: d(CGCAAAAAAGCG) d(GCGTTTTTTCGC) | 2.70 ± 0.38 μM | 0.2 |
8 | 10mer: d(CGCATATGCG)2 | 0.85 ± 0.05 μM | 1.0 |
rbl = ratio of base pairs to ligand. rdl = ratio of duplex to ligand. (–)-Lomaiviticin A (1) was incrementally added to a solution of DNA (2.50 μM/base pair for polynucleotides, 1.25 μM/duplex for oligonucleotides) saturated with thiazole orange (1.25 μM/base pair for polynucleotides, 2.50 μM/duplex for oligonucleotides) at 24 °C. The fluorescence was measured after incubation for 5 min, and the addition of 1 was continued until no further changes in fluorescence were observed.