Abstract
A synthetic route towards a selected set of N-acylated and N-alkylated derivatives of 2 ′-amino-α-L-LNA phosphoramidite building blocks has been developed. Biophysical studies suggest that the 2-oxo-5-azabicyclo[2.2.1]heptane skeleton of 2 ′-amino-α-L-LNA allows precise positioning of intercalators in the core of nucleic acid duplexes.
We greatly appreciate funding from The Danish National Research Foundation.
Notes
a T m values of unmodified duplex (where B = T) toward its complementary DNA and RNA are 28.5°C and 24.5°C, respectively.
b Thermal denaturation temperatures recorded in medium salt buffer ([Na+] = 110 mM, [Cl−] = 100 mM, pH 7.0 (adjusted with 10 mM NaH2PO4/5 mM Na2HPO4)), using 1.0 μM concentrations of the two complementary strands. See synthetic scheme for structure of monomers.