Bioorganic and Medicinal Chemistry Letters p. 73 - 76 (2002)
Update date:2022-08-03
Topics:
Morita, Koji
Hasegawa, Chikako
Kaneko, Masakatsu
Tsutsumi, Shinya
Sone, Junko
Ishikawa, Tomio
Imanishi, Takeshi
Koizumi, Makoto
To develop antisense oligonucleotides, novel nucleosides, 2′-O,4′-C-ethylene nucleosides and their corresponding phosphoramidites, were synthesized as building blocks. The 1H NMR analysis showed that the 2′-O,4′-C-ethylene linkage of these nucleosides restricts the sugar puckering to the N-conformation as well as the linkage of 2′-O,4′-C-methylene nucleosides which are known as bridged nucleic acids (BNA) or locked nucleic acids (LNA). The ethylene-bridged nucleic acids (ENA) showed a high binding affinity for the complementary RNA strand (ΔTm = + 5.2 °C/modification) and were more nuclease-resistant than natural DNA and BNA/LNA. These results indicate that ENA have better properties as antisense oligonucleotides than BNA/LNA.
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