- S-ANTIGEN TRANSPORT INHIBITING OLIGONUCLEOTIDE POLYMERS AND METHODS
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Various embodiments provide STOPS? polymers that are S-antigen transport inhibiting oligonucleotide polymers, processes for making them and methods of using them to treat diseases and conditions. In some embodiments the STOPS? modified oligonucleotides include an at least partially phosphorothioated sequence of alternating A and C units having modifications as described herein. The sequence independent antiviral activity against hepatitis B of embodiments of STOPS? modified oligonucleotides, as determined by HBsAg Secretion Assay, is an EC50 that is less than 100 nM.
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Paragraph 0057; 0348
(2021/06/22)
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- Synthesis and biological properties of chemically modified siRNAs bearing 1-deoxy-d-ribofuranose in their 3′-overhang region
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To elucidate the role of the sugar moiety in the two natural nucleotides of the 3′-overhang region of small interfering RNA (siRNA), we synthesized siRNAs that incorporated two abasic nucleosides, 1-deoxy-d-ribofuranose (R H). We improved the method for preparing an O-protected abasic nucleoside, 1-deoxy-2,3,5-tri-O-benzoyl-β-d-ribofuranose, via the reductive cleavage of the anomeric position of 1-O-acetyl-2,3,5-tri-O-benzoyl-β-d- ribofuranose. To incorporate RH into oligonucleotides by the standard phosphoramidite solid phase method, RH was converted into its phosphoramidite derivative and the solid support linked to a controlled pore glass resin. Chemically modified RNAs possessing RH at the 3′-overhang region were easily prepared in good yields. siRNAs containing RH showed moderate nuclease-resistance and a desirable knockdown effect.
- Taniho, Kazumi,Nakashima, Remi,Kandeel, Mahmoud,Kitamura, Yoshiaki,Kitade, Yukio
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supporting information; experimental part
p. 2518 - 2521
(2012/05/20)
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- New structural motifs for hammerhead ribozymes. Catalytic activity of abasic nucleotide substituted ribozymes
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The synthesis of 1-deoxy-D-ribofuranose-3-(2-cyanoethyl N,N- diisopropylphosphoramidite) (6) from D-ribose and its incorporation into a hammerhead ribozyme is described.
- Beigelman,Karpeisky,Matulic-Adamic,Gonzalez,Usman
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p. 907 - 910
(2007/10/02)
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- Synthesis and characterization of authentic standards for the analysis of ribofuranose-containing carbohydrates by the reductive-cleavage method
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Described herein is the synthesis of all positional isomers of partially methylated and acetylated or benzoylated 1,4-anhydro-D-ribitol.The benzoates are generated simultaneously from 1,4-anhydro-D-ribitol by sequential partial methylation and benzoylation or sequential partial benzoylation and methylation.The individual isomers are obtained in pure form by high-performance liquid chromatography.Debenzoylation and acetylation provided the corresponding acetates.Reported herein are the 1H NMR spectra of the benzoates and the electron-ionization mass spectra of the acetates and the tri-O-methyl derivative and also for the acetates and the tri-O-methyl derivative, their linear temperature programmed gas-liquid chromatography retention indices on three different capillary columns.Keywords: Reductive-cleavage; D-Ribitol, 1,4-anhydro, partially methylated and acylated
- Rozanas, Christine R.,Wang, Nan,Vidlock, Kathy,Gray, Gary R.
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- Transformations of β-Glycofuranosyl Isocyanides into Tetrahydrofurans
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Readily available β-glycofuranosyl isocyanides 1, 2, 4, 5, 6, 18, 19, 20 are transformed into the corresponding protected tetrahydrofurans 21, 22, 23, 24, 25, 26 by means of tributyltin hydride and AIBN.The synthesis of 18 and 19 by dehydration of the for
- Hiebl, Johann,Zbiral, Erich
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p. 683 - 690
(2007/10/02)
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