Abstract
The synthesis of mixed-backbone-oligonucleotides (MBOs) (15 to 25-mers) which contain phosphoric diester (PO) or phosphorothioate (PS) backbones along with segments of internucleotidic O-methylphosphate (POOMe) or O-methylphosphorothioate (PSOMe) linkages have been accomplished using N-pent-4-enoyl ( PNT) nucleoside phosphoramidite synthons. The T ms of the MBOs reveal that they form stable duplexes with complementary DNA and RNA. The MBOs also showed increased resistance to degradation by nucleases. Consequently, the MBOs with methylphosphotriester segments represent a novel class of antisense oligonucleotides with potential for therapeutic and diagnostic applications.
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