OLIGONUCLEOTIDE N3'-P5' PHOSPHORAMIDATES: SYNTHESIS AND COMPOUNDS; HYBRIDIZATION AND NUCLEASE RESISTANCE PROPERTIES

摘要

Modified oligonucleotides 3'-NHP(O)(O-)O-5' phosphoramidates were synthesizedon a solid phase support. The phosphoramidate analogs were found to havesignificantly increased resistance toward phosphodiesterase digestion. Thermaldissociation experiments demonstrated that these compounds form more stableduplexes than phosphodiesters with complementary DNA and particularly RNAstrands. Further, the phosphoramidate analogs can also form stable triplexeswith double-stranded DNA target, where under similar conditions parentphosphodiester compounds failed to do so.