2′-arabino-fluorooligonucleotide N3′→P5′ phosphoramidates: their synthesis and use

摘要

Oligonucleotides with a novel sugar-phosphate backbone containing at least one 2′-arabino-fluoronucleoside and an internucleoside 3′-NH—P(═O)(OR)—O-5′ linkage, where R is a positively charged counter ion or hydrogen, and methods of synthesizing and using the inventive oligonucleotides are provided. The inventive phosphoramidate 2′-aribino-fluorooligonucleotides have a high RNA binding affinity to complementary nucleic acids and are base and acid stable.

主权项

1. A method for inhibiting function of an RNA in a cell, comprising contacting the cell with a polynucleotide that can specifically hybridize with the RNA, wherein the polynucleotide comprises at least one 2′-arabino-fluoronucleoside linked to at least one additional nucleoside subunit by a linkage selected from the group consisting of N3′→P5′ phosphoramidate and N3′→P5′ thiophosphoramidate intersubunit linkages.