- MODIFIED THYMINE POLYNUCLEOTIDE OLIGOMERS AND METHODS
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Disclosed are modified thymine bases that provide enhanced base-pairing affinity for adenine or 2,6-diaminopurine bases in polynucleotide hybridization complexes. Also disclosed are polynucleotide oligomers, polynucleotide hybridization complexes that com
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Paragraph 00202
(2015/11/17)
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- MODIFIED CYTOSINE POLYNUCLEOTIDE OLIGOMERS AND METHODS
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Disclosed are modified cytosine bases that provide enhanced base-pairing affinity for guanine bases in polynucleotide hybridization complexes. Also disclosed are polynucleotide oligomers, polynucleotide hybridization complexes that comprise such modified
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Paragraph 00202
(2015/11/30)
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- Bioreversible protection of nucleoside diphosphates
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(Figure Presented) Going incognito: A new prodrug approach has been developed to facilitate the diffusion of highly polar polyphosphorylated nucleosides across cell membranes (see scheme). Inside the cell, the masking groups on the nucleoside diphosphate
- Jessen, Henning Jacob,Schulz, Tilmann,Balzarini, Jan,Meier, Chris
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supporting information; experimental part
p. 8719 - 8722
(2009/05/15)
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- Synthesis, Bioactivity and Anti-HIV Activity of the Bis(4-acyloxybenzyl) and Mono(4-acylaoxybenzyl) Esters of the 5'-Monophosphate of AZT
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To investigate the design of prodrugs of antiviral nucleosides for targeting to the central nervous system, the bis(4-acyloxybenzyl) esters of the 5'-monophosphate of AZT 5 (R = Me, Et, Pri or But) have been prepared.The reaction of the appropriate bis(4-acyloxybenzyl) N,N-diisopropylphosphoramidite 10 (R = Me, Et, Pri or But) with AZT in the presence of 1H-tetrazole, followed by oxidation of the PIII intermediate with 3-chloroperoxybenzoic acid gave the required triesters 5 in good yield.The lithium salts of the mono(4-acycloxybenzyl) esters of the 5'-phosphate of AZT 7 (R = Me, Et, Pri or But) were prepared by treatment of the triesters 5 with lithium iodide.In the presence of porcine liver carboxyesterase the triesters 5 and diesters 7 decomposed readily to the 5'-monophosphate of AZT 9.The anti-HIV activities of the triesters 5 and diesters 7 were, with one exception, comparable to that of AZT, but the greater cytotoxicity of certain compounds in particular types of cell significantly reduced their selectivity indices.
- Thomson, William,Nicholls, Dave,Irwin, William J.,Al-Mushadani, Julian S.,Freeman, Sally,et al.
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p. 1239 - 1246
(2007/10/02)
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