Abstract
A novel conformationally constrained pyridazinone E(ag)-base PNA-monomer 2 capable of binding thymine in a triplex motif was designed and synthesised. A bis-PNA with the E(ag)-base incorporated in the Hoogsteen strand was hybridised with a complementary DNA. Thermal stability studies revealed an increase in T(m) (4.3 degrees C per mod.) compared to a no-base unit, but showed no improvement over a previously described unconstrained analogue (E, 1). Surprisingly, no significant difference was found in the thermodynamic parameters (DeltaH degrees, DeltaS degrees and DeltaG degrees ) for PNA-DNA triplex formation involving 2 or the unconstrained analogue 1.
| Original language | English |
|---|---|
| Journal | Bioorganic & Medicinal Chemistry Letters |
| Volume | 14 |
| Issue number | 6 |
| Pages (from-to) | 1551-4 |
| Number of pages | 4 |
| ISSN | 0960-894X |
| DOIs | |
| Publication status | Published - 22 Mar 2004 |
Keywords
- Drug Evaluation, Preclinical/methods
- Molecular Structure
- Nucleic Acid Conformation
- Peptide Nucleic Acids/chemistry
- Pyridazines/chemistry
- Thermodynamics
- Thymine/chemistry