NOVEL 2'/3'/5'-(R/S)-SERINYL FUNCTIONALIZED OLIGONUCLEOTIDES

摘要

The present invention provides novel chiral serinyl functionalized tethered oligonucleotides i.e. R/S serinyl functionalized tethered oligonucleotides and the process of preparation thereof. Specifically, the present invention provides a modified nucleoside unit containing the R/S serinyl derivative at 2' of the sugar unit which is introduced in a nucleotide sequence. Also, capping of the oligonucleotides with abasic serinyl derivative to render the nuclease stability to the oligonucleotiedds is also disclosed. The chiral serinyl functionalized tethered oligonucleotides, 2'-O-[R/S-(2-amino-3-methoxy)propyl] nucleic acids with both 3'- and 5'- ends capped with two units of abasic serine have antisense activity against miRNA.