Listar por tema "DERIVATIVES"
Mostrando ítems 1-20 de 23
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Antioxidant activity of a series of fluorinated pyrano-nucleoside analogues of N-4-benzoyl cytosine and N-6-benzoyl adenine
(2007)Fluorinated nucleoside analogues are known as antitumor, antiviral and chemotherapeutic agents, although the antioxidant activity of this kind of molecules is not yet investigated. In this study we have tested the antioxidant ... -
The binding of C5-alkynyl and alkylfurano 2,3-d pyrimidine glucopyranonucleosides to glycogen phosphorylase b: Synthesis, biochemical and biological assessment
(2012)C5-alkynyl and allcylfurano[2,3-d]pyrimidine glucopyranonucleosides have been synthesized and studied as inhibitors of glycogen phosphorylase b (GPb). Kinetic experiments have shown that most of these compounds were low ... -
Branched-chain C-cyano pyranonucleosides: Synthesis of 3 '-C-cyano & 3 '-C-cyano-3 '-deoxy pyrimidine pyranonucleosides as novel cytotoxic agents
(2011)This report describes the total and facile synthesis of 3'-C-cyano & 3'-C-cyano-3'-deoxy pyrimidine pyranonucleosides. Reaction of 3-keto glucoside 1 with sodium cyanide gave the desired precursor 3-C-cyano-1,2:5,6-di-O- ... -
Branched-chain sugar nucleosides: stereocontrolled synthesis and bioevaluation of novel 3 '-C-trifluoromethyl and 3 '-C-methyl pyranonucleosides
(2015)A new series of 3 '-C-trifluoromethyl- and 3 '-C-methyl-beta-D-allopyranonucleosides of 5-fluorouracil and their deoxy derivatives has been designed and synthesized. Treatment of ketosugar 1 with trifluoromethyltrimethylsilane ... -
Correlation between plant growth regulator release rate and bioactivity for the series of newly synthesized phytoactive polymers
(2006)Phytoactive polymers are high molecular weight systems in which a plant growth regulator (PGR) unit is attached to the polymeric chain by a hydrolyzable chemical bond. The release rate of the PGR is linked to the biological ... -
Evaluation of the effectiveness of an ointment based on Alkannins/Shikonins on second intention wound healing in the dog
(2011)The enantiomeric naphthoquinones alkannins and shikonins (A/S) have been established as potent wound healing agents. The purpose of this study was to evaluate the effectiveness of an A/S based ointment for humans on second ... -
A facile, one-step conversion of 6-O-trityl and 6-O-TBDMS monosaccharides into the corresponding formate esters
(2006)A convenient method has been developed for a facile and high-yield conversion of 6-O-tertbutyldimethylsilyl and 6-O-trityl protected monosaccharides to their formate esters, which may serve as useful intermediates for the ... -
Isokinetic knee extension and vertical jumping: Are they related?
(2005)The aim of this study was to examine joint power generation during a concentric knee extension isokinetic test and a squat vertical jump. The isokinetic test joint power was calculated using four different methods. Five ... -
Keto-fluorothiopyranosyl nucleosides: a convenient synthesis of 2-and 4-keto-3-fluoro-5-thioxylopyranosyl thymine analogs
(2011)A novel series of fluorinated keto-beta-D-5-thioxylopyranonucleosides bearing thymine as the heterocyclic base have been designed and synthesized. Deprotection of 3-deoxy-3-fluoro-5-S-acetyl-5-thio-D-xylofuranose (1) and ... -
N-substituted Pyrrole-based Scaffolds as Potential Anticancer and Antiviral Lead Structures
(2015)Undoubtedly, efficient cancer treatment has been a significant challenge for the scientific community over the last decades. Despite tremendous progress made towards this direction, there are still efforts needed to discover ... -
Natural flavonoids as antidiabetic agents. The binding of gallic and ellagic acids to glycogen phosphorylase b
(2015)We present a study on the binding of gallic acid and its dimer ellagic acid to glycogen phosphorylase (GP). Ellagic acid is a potent inhibitor with K(i)s of 13.4 and 7.5 mu M, in contrast to gallic acid which displays K(i)s ... -
A new bifunctional tridentate NSN ligand leading to cationic tricarbonyl fac- M(NSN)(CO)(3) (+) (M = Re, Tc-99m) complexes
(2013)The synthesis and characterization of the new NSN tridentate bifunctional chelating agent 3-[2-(2'-pyridin-2-yl-ethylsulfanyl)ethylamino] propionic acid (as its hydrochloric salt, 1) and of its corresponding rhenium comp ... -
New short route to unsaturated fluoroketonucleosides: Case of 5-fluoro-1-(6-O-acetyl-3,4-di-deoxy-3-fluoro-beta-D-glycero-hex-3-eno-py ranos-2-ulosyl) uracil
(2005)The proposed short synthesis involves two key steps: Oxidation of the isopropylidene derivative of the 3 fluoronucleoside possessing a free hydroxyl group in 2-position and acetylation of deprotected 3-fluoro-2-ketonucleoside ... -
A novel and easy two-step, microwave-assisted method for the synthesis of halophenyl pyrrolo 2,3-b quinoxalines via their pyrrolo precursors. Evaluation of their bioactivity
(2014)A novel, two-step, facile route for the synthesis of pyrrolo[2,3-b]quinoxalines via 2,3-dioxopyrroles, enhanced by microwave irradiation, is presented. The newly synthesized 2,3-dioxo-5-halophenyl pyrrolo precursors 4a-c ... -
Rationally Designed Less Toxic SPD-304 Analogs and Preliminary Evaluation of Their TNF Inhibitory Effects
(2014)SPD-304 was discovered as a promising tumor necrosis factor alpha (TNF) antagonist that promotes dissociation of TNF trimers and therefore blocks the interaction of TNF and its receptor. However, SPD-304 contains a potentially ... -
The s-Hole Phenomenon of Halogen Atoms Forms the Structural Basis of the Strong Inhibitory Potency of C5 Halogen Substituted Glucopyranosyl Nucleosides towards Glycogen Phosphorylase b
(2012)C5 halogen substituted glucopyranosyl nucleosides (1-(beta-D-glucopyranosyl)-5-X-uracil; X=Cl, Br, I) have been discovered as some of the most potent active site inhibitors of glycogen phosphorylase (GP), with respective ... -
STEREOCONTROLLED FACILE SYNTHESIS AND BIOLOGICAL EVALUATION OF (3 ' S) AND (3 ' R)-3 '-AMINO (AND AZIDO)-3 '-DEOXY PYRANONUCLEOSIDES
(2012)This article describes the synthesis of (3'S) and (3'R)-3'-amino-3'-deoxy pyranonucleosides and their precursors (3'S) and (3'R)-3'-azido-3'-deoxy pyranonucleosides. Azidation of 1,2:5,6-di-O-isopropylidene-3-O-toluenesu ... -
Stereocontrolled synthesis of 4 '-C-cyano and 4 '-C-cyano-4 '-deoxy pyrimidine pyranonucleosides as potential chemotherapeutic agents
(2012)A new series of 4'-C-cyano and 4'-C-cyano-4'-deoxy pyrimidine pyranonucleosides has been designed and synthesized. Commercially available 1,2,3,4,6-penta-O-acetyl-D-mannopyranose (1) was condensed with silylated 5-fluorouracil, ... -
Structure based inhibitor design targeting glycogen phosphorylase b. Virtual screening, synthesis, biochemical and biological assessment of novel N-acyl-beta-D-glucopyranosylamines
(2014)Glycogen phosphorylase (GP) is a validated target for the development of new type 2 diabetes treatments. Exploiting the Zinc docking database, we report the in silico screening of 1888 N-acyl-beta-D-glucopyranosylamines ... -
Synthesis and biological evaluation of modified purine homo-N-nucleosides containing pyrazole or 2-pyrazoline moiety
(2014)9-Substituted (pyrazol-5-yl)methyl- or (2-pyrazolin-5-yl)methyl-9H-purines were synthesized from 9-allyl-6-chloro-9H-purine through the 1,3-dipolar cycloaddition reaction with nitrile imines, prepared in situ from the ...