Synthesis and Biological Activity of Phosphoramidimidate and Phosphoramidate DNA
AssigneeThe Regents of the University of Colorado, a body corporate
InventorsAyman Alawneh, Marvin Caruthers
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Abstract
Oligonucleotides comprising phosphoramidimidate internucleotide linkages, and methods of efficiently synthesizing these oligonucleotides with high yield are provided. These oligonucleotides form duplexes with complementary DNA or RNA that are more stable than natural DNA or DNA/RNA complexes, are active with RNAse H1, and may be transfected into cells using standard lipid reagents. These analogues are therefore useful for numerous therapeutic antisense applications.
Claims18
An oligomer comprising a monomer subunit comprising the chemical structure of formula I:
- wherein:
- each B is independently a nucleic acid base (adenosine, guanosine, uracil, thymine, cytosine, inosine), or a nucleic acid base protected with a silyl protecting group or an acid-labile or base-labile protecting group.
A phosphoramidimidate synthon having a chemical structure:
- wherein:
- each B2 is independently a nucleic acid base (adenosine, guanosine, uracil, thymine, cytosine, inosine), or a nucleic acid base protected with a silyl protecting group or an acid-labile or base-labile protecting group.
Dependencies are inferred from the claim text.