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Recent advances in S-adenosyl-L-homocysteine hydrolase inhibitors and their potential clinical applications
The increased understanding of the biochemical properties and mechanisms of catalysis mediated by SAH hydrolase has been to generate more potent and more specific inhibitors of the enzyme. Expand
Two distinct molecular mechanisms underlying cytarabine resistance in human leukemic cells.
Two resistant derivatives of the human leukemic line CCRF-CEM were obtained by stepwise selection in different concentrations of AraC, pointing to at least two distinct mechanisms of Ara C resistance inLeukemic cells. Expand
Nucleic acid related compounds. 34. Non-aqueous diazotization with tert-butyl nitrite. Introduction of fluorine, chlorine, and bromine at C-2 of purine nucleosides
Treatment of 2,6-diamino-9-(2,3,5-tri-O-acetyl-β-D-ribofuranosyl)purine (1c) with tert-butyl nitrite (TBN) in 60% anhydrous hydrogen fluoride/pyridine at −20 °C gave 2-fluoroadenosine triacetate (2...
The crystal and molecular structure of 5-(propyn-1-yl)-1-(β-D-arabinofuranosyl)uracil. A very short C≡C triple bond
The crystal structure of 5-(propyn-1-yl)-1-(β-D-arabinofuranosyl)uracil, an analog of the active antiherpes nucleoside 1-(β-D-arabinofuranosyl)thymine, was determined by X-ray diffraction. The… Expand
Mild and efficient functionalization at C6 of purine 2'-deoxynucleosides and ribonucleosides.
[reaction: see text] Treatment of sugar-protected inosine and 2'-deoxyinosine derivatives with a cyclic secondary amine or imidazole and I(2)/Ph(3)P/EtN(i-Pr)(2)/(CH(2)Cl(2) or toluene) gave… Expand
2'-Deoxy-2'-methylenecytidine and 2'-deoxy-2',2'-difluorocytidine 5'-diphosphates: potent mechanism-based inhibitors of ribonucleotide reductase.
- C. H. Baker, J. Banzon, +6 authors R. Resvick
- Chemistry, Medicine
- Journal of medicinal chemistry
- 1 June 1991
The analogous RDPR of mammalian cells should be regarded as a likely target and/or activating enzyme for these novel mechanism-based inactivators of Escherichia coli ribonucleoside diphosphate reductase. Expand
Nucleic acid related compounds. 11. Adenosine 2',3'-ribo-epoxide. Synthesis, intramolecular degradation, and transformation into 3'-substituted xylofuranosyl nucleosides and the lyxo-epoxide.
Uridine binding motifs of human concentrative nucleoside transporters 1 and 3 produced in Saccharomyces cerevisiae.
The binding profiles identified in this study can be used to predict the potential transportability of nucleoside analogs, including anticancer or antiviralucleoside drugs, by hC NT1 and hCNT3. Expand
Uridine Binding and Transportability Determinants of Human Concentrative Nucleoside Transporters
- J. Zhang, Kyla M. Smith, +8 authors C. Cass
- Chemistry, Medicine
- Molecular Pharmacology
- 1 September 2005
The transportability profiles identified in this study should prove useful in the development of anticancer and antiviral therapies with nucleoside drugs that are permeants of members of the hCNT protein family. Expand
A Refined Model of the HCV NS5A Protein Bound to Daclatasvir Explains Drug-Resistant Mutations and Activity against Divergent Genotypes
- K. Barakat, Anwar Anwar-mohamed, J. Tuszynski, M. Robins, D. Tyrrell, M. Houghton
- Biology, Computer Science
- J. Chem. Inf. Model.
- 23 February 2015
The proposed model is the first to reveal the detailed binding mode of Daclatasvir and provides a tool to facilitate design of second generation drugs, which may confer less resistance and/or broader activity against HCV. Expand