Πλοήγηση ανά Θέμα "BIOLOGICAL EVALUATION"
Αποτελέσματα 1-19 από 19
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1-(3-Deoxy-3-fluoro-beta-D-glucopyranosyl) pyrimidine derivatives as inhibitors of glycogen phosphorylase b: Kinetic, crystallographic and modelling studies
(2010)Design of inhibitors of glycogen phosphorylase (GP) with pharmaceutical applications in improving glycaemic control in type 2 diabetes is a promising therapeutic strategy. The catalytic site of muscle glycogen phosphorylase ... -
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 ... -
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 ... -
Curcumin analogues as possible anti-proliferative & anti-inflammatory agents
(2011)A series of novel curcumin analogues has been designed, synthesized and tested in vitro/in vivo as potential multi-target agents. Their anti-proliferative and anti-inflammatory activities were studied. Compounds 1b and 2b ... -
Efficient synthesis of exomethylene- and keto-exomethylene-D-glucopyranosyl nucleoside analogs as potential cytotoxic agents
(2011)A novel series of exomethylene- and keto-exomethylene-D-glucopyranonucleosides with thymine, uracil, and 5-fluorouracil as heterocyclic bases have been designed and synthesized. Wittig condensation of the 3-keto glucoside ... -
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 ... -
Kinetic and in silico analysis of the slow-binding inhibition of human poly(A)-specific ribonuclease (PARN) by novel nucleoside analogues
(2012)Poly(A)-specific ribonuclease (PARN) is a 3'-exoribonuclease that efficiently degrades poly(A) tails and regulates, in part, mRNA turnover rates. We have previously reported that adenosine- and cytosine-based glucopyranosyl ... -
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 products and their derivatives as inhibitors of glycogen phosphorylase: potential treatment for type 2 diabetes
(2014)Glycogen phosphorylase (GP) (EC 2.4.1.1) is an important therapeutic target for the potential treatment of type 2 diabetes. The search for potent, selective and drug-like GP inhibitors which may eventually lead to hypoglycaemic ... -
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 ... -
Novel conformationally constrained pyrazole derivatives as potential anti-cancer agents
(2015)The synthesis of 17 novel conformationally constrained pyrazole derivatives is reported herein, along with the assessment of their anti-proliferative and anti-angiogenic activities. The evaluation of their inhibitory effect ... -
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, ... -
Stereoselective facile synthesis of 2 '-spiro pyrimidine pyranonucleosides via their key intermediate 2 '-C-cyano analogues. Evaluation of their bioactivity
(2014)A novel series of 2'-spiro pyrimidine pyranonucleosides has been designed and synthesized. Their precursors, 2'-C-cyano nucleosides 5a,b and 6a,b, were obtained by subjecting 1a,b to the sequence of selective protection ... -
Synthesis and molecular modelling of unsaturated exomethylene pyranonucleoside analogues with antitumor and antiviral activities
(2008)This report describes the total and facile synthesis of the unsaturated keto and exomethylene pyranonucleoside analogues, 1-(2,3,4-trideoxy-4-methylene-6-O-trityl-alpha-D-glycero-hex-2-enopyranosyl)uracil (10), ... -
Synthesis of 3-fluoro-6-S-(2-S-pyridyl) nucleosides as potential lead cytostatic agents
(2010)The 3-deoxy-3-fluoro-6-S-(2-S-pyridyl)-6-thio-beta-D-glucopyranosyl nucleoside analogs 7 were prepared via two facile synthetic routes. Their precursors, 3-fluoro-6-thio-glucopyranosyl nucleosides 5a-e, were obtained by ... -
Synthesis of 4,6-dideoxy-3-fluoro-2-keto-beta-D-glucopyranosyl analogues of 5-fluorouracil, N-6-benzoyl adenine, uracil, thymine, N-4-benzoyl cytosine and evaluation of their antitumor activities
(2010)The synthesis of the unsaturated 4,6-dideoxy-3-fluoro-2-keto-beta-D-glucopyranosyl nucleosides of 5-fluorouracil (6a), N-6-benzoyl adenine (6b), uracil (6c), thymine (6d) and N-4-benzoyl cytosine (6e), is described. ... -
Synthesis of Novel Thiopurine Pyranonucleosides: Evaluation of Their Bioactivity
(2015)We report the synthesis of novel thiopurine pyranonucleosides. Direct coupling of silylated 6-mercaptopurine and 6-thioguanine with the appropriate pyranoses 1a-e via Vorbruggen nucleosidation, gave the N-9 linked ... -
Unsaturated dideoxy fluoro-ketopyranosyl nucleosides as new cytostatic agents: A convenient synthesis of 2,6-dideoxy-3-fluoro-4-keto-beta-D-glucopyranosyl analogues of uracil, 5-fluorouracil, thymine, N-4-benzoyl cytosine and N-6-benzoyl adenine
(2009)The beta-protected nucleosides of uracil (2a), 5-fluorouracil (2b), thymine (2c), N-4-benzoyl cytosine (2d) and N-6-benzoyl adenine (2e) were synthesized by condensation of the peracetylated 3-deoxy-3-fluoro-D-glucopyramose ...