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Showing 1 to 20 of 200 for “"nucleoside"”.
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Synthesis of nucleoside analogues.
A basic introduction to a variety of nucleoside derivatives is described along with a selection of recent syntheses of the said compounds. Initial studies on the synthesis of the key furan based intermediate N-2,5-dihydro-5-(2,2-dimethyl-1,3-dioxolan-4-yl)furanyl trichloroacetamide which when …
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Synthesis of Novel Cyclobutane Nucleoside Analogues
A synthesis of cyclobutane nucleosides is described. The method involved the triflation of a -hydroxymethyl-cyclobutanone and its subsequent displacement by a 6-chloropurinyl anion to generate N-7 and N-9 regioisomers. The stereoselective reduction of the N-alkylated ketones yielded the …
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Structural and Functional Studies of Nucleoside Transporters
<p>Nucleoside transport is required for the salvage pathway of DNA and RNA, provides a transport route for nucleoside-like drugs and regulates adenosine signaling. The eukaryotic cell possesses two evolutionarily unrelated protein families of nucleoside transporters, the concentrative nucleoside …
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Flavonoids and Related Compounds as Nucleoside Transporter Inhibitors
<p>Mammalian nucleoside transporters can be classified into two main categories, namely, equilibrative nucleoside transporters (ENTs) and concentrative nucleoside transporters (CNTs). ENTs are ubiquitous, and mediate sodium-independent bi-directional facilitated diffusion nucleoside transport …
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Nucleoside and oligonucleotide approaches towards potential HIV chemotherapies
… which were developed for the synthesis of nucleoside intermediates for oligonucleotide applications were also used to prepare a series of nucleoside analogues derived from uridine, 2'-deoxyuridine and AZT. Crystal structures of six compounds were successfully determined. Anti-HIV activity …
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STRUCTURE-FUNCTION ANALYSIS OF THE HUMAN EQUILIBRATIVE NUCLEOSIDE TRANSPORTER 1
… domains 1 and 2 of the human equilibrative nucleoside transporter 1 (hENTl), in order to assess their contributions to transporter functionality. Through affinity changes in [ H]NBMPR binding, competitive inhibition profiles with ENT1 inhibitors and [ H]2- chloroadenosine uptake, these …
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Investigating Mechanisms of Nucleoside Reverse Transcriptase Inhibitor Induced Sensory Neuropathy
… idea that the ART may cause PSN. Although the nucleoside reverse transcriptase inhibitors (NRTIs) used in the ART are thought to contribute to PSN, the mechanisms underlying the PSN induced by NRTIs are unclear. This is partly due to the lack of a good model for mechanistic investigations. In …
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The Impact of Nucleoside Sugar Modification on Biochemical DNA Transactions
… for the synthesis of oligonucleotides with nucleoside analogues with biased sugar conformations at the 3'-end (growing end) as well as at internucleotide positions. Through a series of thermodynamic, structural and functional studies, we reveal how sugar structure and conformational …
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Spectroscopic analysis and synthesis of nucleoside analogs for lethal mutagenesis
… to existing therapeutics. A novel antiviral nucleoside analog, 5-Aza-5,6-dihydro-2'- deoxycytidine (KP1212), employs the mechanism of lethal mutagenesis to avoid the problem of drug resistance and use the virus's high mutation rate against it. KP1212 is incorporated into DNA by HIV reverse …
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Application of thermodynamic principles in biocatalytic synthesis of novel nucleoside analogues
Nucleosides and analogues thereof are central molecules in modern cancer therapy and in the fight against viral infections. However, their efficient synthesis is a challenging task for synthetic chemistry. This necessitates lengthy routes and results in low atom economy. Nature’s chemistry set, on …
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Molecular investigation if the rat jejunal active nucleoside transport protein rCNT1
Active, sodium-dependent nucleoside transport systems have been kinetically described in a number of different mammalian tissues. The recent cloning of several active, mammalian nucleoside transporters belonging to a novel gene family has provided an opportunity to examine both the …
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Synthetic efforts towards the total synthesis of the Nucleoside Antibiotic, (+)-Amicetin
(+)-Amicetin is a hexopyranosyl cytosine, a relatively unexplored class of RNA-binding natural products, which are a sub-group of peptidyl transferase antibiotics. As a peptidyl transferase antibiotic, (+)-Amicetin acts as a universal antibiotic, however it has been shown to be particularly …
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Synthesis and Biological Evaluation of Modified Adenosine and Thymidine Nucleoside Analogues
SAMENVATTING In Deel I (Hoofdstuk 1-2) van dit werk beschreven we de synthese van gemodificeerde adenosine en thymidine analogen (zie Figuur 1). Deze verbindingen werden als moleculaire probes gebruikt voor de biologische evaluatie van adenosine-receptoren (ARn, Deel II, Hoofdstuk 3-6), die behoren …
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Equilibrative Nucleoside Transporter Mediated Drug Disposition Across the Blood-Testis Barrier
… and chemotherapeutic agents are classified as nucleoside analogs, which resemble endogenous nucleosides essential for nucleic acid synthesis and spermatogenesis. Due to similarity in chemical structure, these drugs are suspected to be substrates of the equilibrative nucleoside transporters …
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Syntheses of Fluorescent Base, Nucleoside, and Nucleotide Analogues: Linear-Benzopurine Derivatives
Made available in DSpace on 2014-12-13T20:10:43Z (GMT). No. of bitstreams: 1 8004204.pdf: 2095606 bytes, checksum: fd0734fb680ef4f81c04a94ce0b64e7f (MD5) Previous issue date: 1979
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The Synthesis and Studies of Some Adenine Nucleoside and Nucleotide Analogs
Made available in DSpace on 2014-12-10T23:00:55Z (GMT). No. of bitstreams: 1 7105227.pdf: 3677059 bytes, checksum: f0eb84f55cac8951f448deefba203a90 (MD5) Previous issue date: 1970
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