N2′-Functionalized 2′-Amino-α-L-LNA Adenine Derivatives—Efficient Targeting of Single Stranded DNA

Abstract

The synthesis of two pyrene-functionalized 2′-amino-α-L-LNA adenine building blocks is outlined and initial results from thermal denaturation studies are presented.

Keywords:

• Conformationally restricted nucleosides
• antisense
• antigene

The Danish National Research Foundation is thanked for financial support.

Notes

^a T _m values/°C (Δ T _m = change in T _m value calculated relative to DNA:DNA or DNA:RNA reference duplex) recorded in medium salt buffer ([Na⁺] = 110 mM, [Cl⁻] = 100 mM, pH 7.0 (NaH₂PO₄/Na₂HPO₄)), using 1.0 μM concentrations of each strand. T _m values (°C) of ON1 and ON2 towards DNA strands containing a single mismatch in the central position A/C/G: 18.5/27.0/19.5 and 18.0/27.0/22.0, respectively. T _m values (°C) of ON1 and ON2 towards RNA strands containing a single mismatch in the central position A/C/G: 13.5/16.0/14.0 and 16.5/16.0/13.5, respectively.