High-affinity peptide nucleic acid oligomers containing tricyclic cytosine analogues

Org Lett. 2002 Dec 12;4(25):4395-8. doi: 10.1021/ol027026a.

Abstract

[structure: see text] Peptide nucleic acid (PNA) monomers containing the tricyclic cytosine analogues phenoxazine, 9-(2-aminoethoxy)phenoxazine (G-clamp), and 9-(3-aminopropoxy)phenoxazine (propyl-G-clamp) have been synthesized. The modified nucleobases were incorporated into PNA oligomers using Boc-chemistry for solid-phase synthesis. PNAs containing single G-clamp modifications exhibit significantly enhanced affinity toward RNA and DNA targets relative to unmodified PNA while maintaining mismatch discrimination. These PNA G-clamp modifications exhibit the highest increase in affinity toward nucleic acid targets reported so far for PNA modifications.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cytosine / analogs & derivatives*
  • Cytosine / chemistry*
  • DNA / chemistry
  • DNA / metabolism
  • Molecular Structure
  • Oxazines / chemistry
  • Peptide Nucleic Acids / chemical synthesis*
  • Peptide Nucleic Acids / chemistry*
  • RNA / chemistry
  • RNA / metabolism

Substances

  • 9-(2-aminoethoxy)phenoxazine
  • 9-(3-aminopropoxy)phenoxazine
  • Oxazines
  • Peptide Nucleic Acids
  • RNA
  • Cytosine
  • DNA
  • phenoxazine