A1 Vertaisarvioitu alkuperäisartikkeli tieteellisessä lehdessä
Towards oligonucleotide pro-drugs: 2,2-bis(ethoxycarbonyl) and 2-(alkylaminocarbonyl)-2-cyano substituted 3-(pivaloyloxy)propyl groups as biodegradable protecting groups for internucleosidic phosphoromonothioate
Tekijät: Poijarvi P, Oivanen M, Lonnberg H
Kustantaja: BENTHAM SCIENCE PUBL LTD
Julkaisuvuosi: 2004
Lehti:: Letters in Organic Chemistry
Tietokannassa oleva lehden nimi: LETTERS IN ORGANIC CHEMISTRY
Lehden akronyymi: LETT ORG CHEM
Vuosikerta: 1
Numero: 2
Aloitussivu: 183
Lopetussivu: 188
Sivujen määrä: 6
ISSN: 1570-1786
DOI: https://doi.org/10.2174/1570178043488536
Tiivistelmä
The applicability of 2.2-bis(ethoxycarbonyl)-3-(pivaloyloxy)propyl and 2-cyano-2-(2-phenylethylaminocarbonyl)-3-(pivaloyloxy)propyl groups as biodegradable protecting agents for the internucleosidic linkages of phosphorothioate antisense oligonucleotides has been studied. For this purpose, protected phosphoromonothioates of thymidylyl-(3'-->5')-thymidine [Tp(s)T] containing either a bridged or non-bridged sulfur atom have been prepared. and their chemical stability and enzymatic deprotection have been studied.
The applicability of 2.2-bis(ethoxycarbonyl)-3-(pivaloyloxy)propyl and 2-cyano-2-(2-phenylethylaminocarbonyl)-3-(pivaloyloxy)propyl groups as biodegradable protecting agents for the internucleosidic linkages of phosphorothioate antisense oligonucleotides has been studied. For this purpose, protected phosphoromonothioates of thymidylyl-(3'-->5')-thymidine [Tp(s)T] containing either a bridged or non-bridged sulfur atom have been prepared. and their chemical stability and enzymatic deprotection have been studied.
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