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

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....

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Bibliographic Details
Main Authors Gryaznov, Sergei, Schultz, Ronald G
Format Patent
LanguageEnglish
Published 02.08.2011
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Summary: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′-arabino-fluorooligonucleotides have a high RNA binding affinity to complementary nucleic acids and are base and acid stable.