Parcourir par auteur "Kiritsis, C."
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3 '-Axial CH2OH Substitution on Glucopyranose does not Increase Glycogen Phosphorylase Inhibitory Potency. QM/MM-PBSA Calculations Suggest Why
Manta, S.; Xipnitou, A.; Kiritsis, C.; Kantsadi, A. L.; Hayes, J. M.; Skamnaki, V. T.; Lamprakis, C.; Kontou, M.; Zoumpoulakis, P.; Zographos, S. E.; Leonidas, D. D.; Komiotis, D. (2012)Glycogen phosphorylase is a molecular target for the design of potential hypoglycemic agents. Structure-based design pinpointed that the 3'-position of glucopyranose equipped with a suitable group has the potential to form ... -
The binding of C5-alkynyl and alkylfurano 2,3-d pyrimidine glucopyranonucleosides to glycogen phosphorylase b: Synthesis, biochemical and biological assessment
Kantsadi, A. L.; Manta, S.; Psarra, A. M. G.; Dimopoulou, A.; Kiritsis, C.; Parmenopoulou, V.; Skamnaki, V. T.; Zoumpoulakis, P.; Zographos, S. E.; Leonidas, D. D.; Komiotis, D. (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
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- ... -
Comparison of the Growth Curves of Cancer Cells and Cancer Stem Cells
Toloudi, M.; Ioannou, E.; Chatziioannou, M.; Apostolou, P.; Kiritsis, C.; Manta, S.; Komiotis, D.; Papasotiriou, I. (2014)A fundamental problem in cancer research is identification of the cells responsible for tumor formation. The latest field of cancer research has revealed the existence and role of cancer stem cells (CSCs). These findings ... -
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 ... -
Keto and Exomethylene Pyranonucleosides as Antitumor Agents
Tsoukala, E.; Manta, S.; Kiritsis, C.; Komiotis, D. (2012)Nucleosides and their analogues take an important place in medicinal chemistry as the structural basis for the development of therapeutic agents. Recently, there has been a renewed interest in the synthesis of keto and ... -
Keto-fluorothiopyranosyl nucleosides: a convenient synthesis of 2-and 4-keto-3-fluoro-5-thioxylopyranosyl thymine analogs
Tsoukala, E.; Manta, S.; Tzioumaki, N.; Kiritsis, C.; Komiotis, D. (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 ... -
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 ... -
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
Kantsadi, A. L.; Hayes, J. M.; Manta, S.; Skamnaki, V. T.; Kiritsis, C.; Psarra, A. M. G.; Koutsogiannis, Z.; Dimopoulou, A.; Theofanous, S.; Nikoleousakos, N.; Zoumpoulakis, P.; Kontou, M.; Papadopoulos, G.; Zographos, S. E.; Komiotis, D.; Leonidas, D. D. (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
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 ... -
Study of the interaction among Notch pathway receptors, correlation with stemness, as well as their interaction with CD44, dipeptidyl peptidase-IV, hepatocyte growth factor receptor and the SETMAR transferase, in colon cancer stem cells
Apostolou, P.; Toloudi, M.; Ioannou, E.; Kourtidou, E.; Chatziioannou, M.; Kopic, A.; Komiotis, D.; Kiritsis, C.; Manta, S.; Papasotiriou, I. (2013)Context: The Notch signaling pathway is one of the most important pathways during normal development and implicated in self-renewal of adult stem cells and differentiation of progenitor cells. Abnormal expression of Notch ... -
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 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. ... -
Unsaturation: An important structural feature to nucleosides' antiviral activity
Manta, S.; Kiritsis, C.; Dimopoulou, A.; Parmenopoulou, V.; Kollatos, N.; Tsotinis, A.; Komiotis, D. (2014)In the search of effective, selective and nontoxic antiviral agents, a variety of nucleoside analogues have been synthesized, with different functionalities in the carbohydrate moiety and/or the heterocyclic base. Nucleoside ...