Listar por autor "Balzarini, J."
Mostrando ítems 1-16 de 16
-
Branched-chain C-cyano pyranonucleosides: Synthesis of 3 '-C-cyano & 3 '-C-cyano-3 '-deoxy pyrimidine pyranonucleosides as novel cytotoxic agents
Kiritsis, C.; Manta, S.; Parmenopoulou, V.; Balzarini, J.; Komiotis, D. (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- ... -
Dideoxy fluoro-ketopyranosyl nucleosides as potent antiviral agents: Synthesis and biological evaluation of 2,3-and 3,4-dideoxy-3-fluoro-4-and-2-keto-beta-D-glucopyranosyl derivatives of N-4-benzoyl cytosine
Manta, S.; Tsoukala, E.; Tzioumaki, N.; Goropevsek, A.; Pamulapati, R. T.; Cencic, A.; Balzarini, J.; Komiotis, D. (2009)The synthesis of the dideoxy fluoro ketopyramonucleoside analogues, 1-(2,3-dideoxy-3-fluoro-6-O-trityl-beta-D-glycero-hexopyranosyl-4-ulose)-N-4-benzoyl cytosine (7a), 1-(3,4-dideoxy-3-fluoro-6-O-trityl-beta-D-glycero-he ... -
Efficient synthesis of exomethylene- and keto-exomethylene-D-glucopyranosyl nucleoside analogs as potential cytotoxic agents
Tzioumaki, N.; Tsoukala, E.; Manta, S.; Kiritsis, C.; Balzarini, J.; Komiotis, D. (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 ... -
N-substituted Pyrrole-based Scaffolds as Potential Anticancer and Antiviral Lead Structures
Pegklidou, K.; Papastavrou, N.; Gkizis, P.; Komiotis, D.; Balzarini, J.; Nicolaou, I. (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 ... -
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
Manta, S.; Gkaragkouni, D. N.; Kaffesaki, E.; Gkizis, P.; Hadjipavlou-Litina, D.; Pontiki, E.; Balzarini, J.; Dehaen, W.; Komiotis, D. (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 ... -
Rapid microwave-enhanced synthesis of C5-alkynyl pyranonucleosides as novel cytotoxic antitumor agents
Dimopoulou, A.; Manta, S.; Kiritsis, C.; Gkaragkouni, D. N.; Papasotiriou, I.; Balzarini, J.; Komiotis, D. (2013)A microwave-assisted, one-pot, coupling reaction for the synthesis of C5-alkynyl-uracil and cytosine glucopyranonucleosides has been developed. The reaction is carried out under standard Sonogashira coupling conditions ... -
STEREOCONTROLLED FACILE SYNTHESIS AND BIOLOGICAL EVALUATION OF (3 ' S) AND (3 ' R)-3 '-AMINO (AND AZIDO)-3 '-DEOXY PYRANONUCLEOSIDES
Manta, S.; Parmenopoulou, V.; Kiritsis, C.; Dimopoulou, A.; Kollatos, N.; Papasotiriou, I.; Balzarini, J.; Komiotis, D. (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
Kiritsis, C.; Manta, S.; Parmenopoulou, V.; Dimopoulou, A.; Kollatos, N.; Papasotiriou, I.; Balzarini, J.; Komiotis, D. (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
Kiritsis, C.; Manta, S.; Dimopoulou, A.; Parmenopoulou, V.; Gkizis, P.; Balzarini, J.; Komiotis, D. (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 Biological Evaluation of 3 '-C-Ethynyl and 3 '-C-(1,4-disubstituted-1,2,3-triazolo) Double-Headed Pyranonucleosides
Kiritsis, C.; Manta, S.; Papasotiriou, I.; Coutouli-Argyropoulou, E.; Trakossas, S.; Balzarini, J.; Komiotis, D. (2012)A novel series of 3'-C-ethynyl and 3'-C-(1,4-disubstituted-1,2,3-triazolo) double-headed pyranonucleosides has been designed and synthesized. Reaction of 3-keto glucoside 1 with ethynyl magnesium bromide gave the desired ... -
Synthesis and biological evaluation of 3′-c-ethynyl and 3′-c-(1,4-disubstituted-1,2,3-triazolo) double-headed pyranonucleosides
Kiritsis, C.; Manta, S.; Papasotiriou, I.; Coutouli-Argyropoulou, E.; Trakossas, S.; Balzarini, J.; Komiotis, D. (2012)A novel series of 3′-C-ethynyl and 3′-C-(1,4-disubstituted-1,2, 3-triazolo) double-headed pyranonucleosides has been designed and synthesized. Reaction of 3-keto glucoside 1 with ethynyl magnesium bromide gave the desired ... -
Synthesis and biological evaluation of unsaturated keto and exomethylene D-arabinopyranonucleoside analogs: Novel 5-fluorouracil analogs that target thymidylate synthase
Tzioumaki, N.; Manta, S.; Tsoukala, E.; Voorde, J. V.; Liekens, S.; Komiotis, D.; Balzarini, J. (2011)The synthesis of pyrimidine unsaturated keto and exomethylene arabinopyranonucleoside analogs as potential antitumor and antiviral agents is described. Commercially available 1,2,3,4-tetra-O-acetyl-D-arabinopyranose (1) ... -
Synthesis of 3-fluoro-6-S-(2-S-pyridyl) nucleosides as potential lead cytostatic agents
Tsoukala, E.; Tzioumaki, N.; Manta, S.; Riga, A.; Balzarini, J.; Komiotis, D. (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
Manta, S.; Tsoukala, E.; Tzioumaki, N.; Kiritsis, C.; Balzarini, J.; Komiotis, D. (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, Antiviral and Cytostatic Evaluation of Unsaturated Exomethylene and Keto D-Lyxopyranonucleoside Analogues
Tzioumaki, N.; Tsoukala, E.; Manta, S.; Agelis, G.; Balzarini, J.; Komiotis, D. (2009)This report describes the synthesis of unsaturated exomethylene lyxopyranonucleoside analogues as potential biologically active agents. Commercially available 1,2,3,4-tetra-O-acetyl-alpha-D-lyxopyranose 1 was condensed ... -
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
Manta, S.; Tzioumaki, N.; Tsoukala, E.; Panagiotopoulou, A.; Pelecanou, M.; Balzarini, J.; Komiotis, D. (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 ...