RNAs Containing Carbocyclic Ribonucleotides

Org Lett. 2022 Jan 21;24(2):525-530. doi: 10.1021/acs.orglett.1c03936. Epub 2021 Dec 27.

Abstract

Toward the goal of evaluation of carbocyclic ribonucleoside-containing oligonucleotide therapeutics, we developed convenient, scalable syntheses of all four carbocyclic ribonucleotide phosphoramidites and the uridine solid-support building block. Crystallographic analysis confirmed configuration and stereochemistry of these building blocks. Duplexes with carbocyclic RNA (car-RNA) modifications in one strand were less thermodynamically stable than duplexes with unmodified RNA. However, circular dichroism spectroscopy indicated that global conformations of the duplexes containing car-RNAs were similar to those in the unmodified duplexes.

MeSH terms

  • Circular Dichroism
  • Molecular Structure
  • Nucleic Acid Conformation
  • Organophosphorus Compounds / chemical synthesis
  • Organophosphorus Compounds / chemistry
  • RNA* / chemistry
  • Ribonucleotides* / chemical synthesis
  • Ribonucleotides* / chemistry
  • Uridine / analogs & derivatives
  • Uridine / chemical synthesis
  • Uridine / chemistry

Substances

  • RNA
  • Ribonucleotides
  • Organophosphorus Compounds
  • Uridine
  • phosphoramidite