Now showing items 176-195 of 387

    • Kinetic Resolution of Allyltriflamides through a Pd-Catalyzed C–H Functionalization with Allenes: Asymmetric Assembly of Tetrahydropyridines 

      González González, José Manuel; Cendón Mariño, Borja; Mascareñas Cid, José Luis; Gulías Costa, Moisés (American Chemical Society, 2021)
      Enantioenriched, six-membered azacycles are essential structural motifs in many products of pharmaceutical or agrochemical interest. Here we report a simple and practical method for enantioselective assembly of ...
    • Lanthanide-based peptide biosensor to monitor CDK4/cyclin D kinase activity 

      González-Vera, Juan A.; Bouzada, David; Bouclier, Céline; Vázquez Sentís, Marco Eugenio; Morris, May C. (Royal Society of Chemistry, 2017)
      We describe a lanthanide biosensor that responds to CDK4 kinase activity in melanoma cell extracts through a significant and dose dependent increase in luminescence, thanks to sensitization of a DOTA[Tb3+] complex incorporated ...
    • Light-Controlled Cellular Internalization and Cytotoxicity of Nucleic Acid-Binding Agents: Studies in Vitro and in Zebrafish Embryos 

      Penas Tallón, Cristina; Sánchez López, Mateo Isidro; Guerra Varela, Jorge; Sánchez Piñón, Laura; Vázquez Sentís, Marco Eugenio; Mascareñas Cid, José Luis (Wiley, 2016)
      We synthesized octa‐arginine conjugates of DNA‐binding agents (bisbenzamidine, acridine and Thiazole Orange) and demonstrated that their DNA binding and cell internalization can be inhibited by appending a (negatively ...
    • Liver X receptor activation with an intranasal polymer therapeutic prevents cognitive decline without altering lipid levels 

      Navas Guimaraes, María Eugenia; López Blanco, Roi; Correa Chinea, Juan Francisco; Fernández Villamarín, Marcos; Bistué, María Beatriz; Martino Adami, Pamela; Morelli, Laura; Kumar, Vijay; Wempe, Michael F.; Cuello, A. Claudio; Fernández Megía, Eduardo; Bruno, Martín Alejandro (ACS, 2021)
      The progressive accumulation of amyloid-beta (Aβ) in specific areas of the brain is a common prelude to late-onset of Alzheimer’s disease (AD). Although activation of liver X receptors (LXR) with agonists decreases Aβ ...
    • LN-1-255, a penicillanic acid sulfone able to inhibit the class D carbapenemase OXA-48 

      Vallejo Vidal, Juan Andrés; Martínez Guitián, Marta; Vázquez Ucha, Juan Carlos; González Bello, Concepción; Poza, Margarita; Buynak, John; Bethel, Christopher R.; Bonomo, Roberto A.; Bou, Germán; Beceiro Casas, Alejandro (Oxford University Press, 2016-04-28)
      Objectives Carbapenemases are the most important mechanism responsible for carbapenem resistance in Enterobacteriaceae. Among carbapenemases, OXA-48 presents unique challenges as it is resistant to β-lactam inhibitors. ...
    • Mapping a protein recognition centre with chiral photoactive ligands. An integrated approach combining photophysics, reactivity, proteomics and molecular dynamics simulation studies 

      Limones Herrero, Daniel; Pérez Ruiz, Raúl; Lence Quintana, Emilio José; González Bello, Concepción; Miranda, Miguel A.; Jiménez, Consuelo M. (Royal Society of Chemistry, 2017-01-05)
      A multidisciplinary strategy to obtain structural information on the intraprotein region is described here. As probe ligands, (S)- and (R)-CPFMe (the methyl esters of the chiral drug carprofen) have been selected, while ...
    • Mechanistic Basis of the Inhibition of Type II Dehydroquinase by (2S)- and (2R)-2-Benzyl-3-dehydroquinic Acids 

      Lence Quintana, Emilio José; Tizón, Lorena; Otero Casas, José Manuel; Peón López, Antonio; Prazeres, Verónica F. V.; Llamas Saiz, Antonio Luis; Fox, Gavin V.; Raaij, Mark J. van; Lamb, Heather; Hawkins, Alastair R.; González Bello, Concepción (American Chemical Society, 2013)
      The structural changes caused by the substitution of the aromatic moiety in (2S)-2-benzyl-3-dehydroquinic acids and its epimers in C2 by electron-withdrawing or electron-donating groups in type II dehydroquinase enzyme ...
    • Mechanistic insight into the reaction catalysed by bacterial type II dehydroquinases 

      Coderch, Claire; Lence Quintana, Emilio José; Peón López, Antonio; Lamb, Heather; Hawkins, Alastair R.; Gago, Federico; González Bello, Concepción (Portland Press, 2014-03-15)
      DHQ2 (type II dehydroquinase), which is an essential enzyme in Helicobacter pylori and Mycobacterium tuberculosis and does not have any counterpart in humans, is recognized to be an attractive target for the development ...
    • Membrane-disrupting iridium(III) oligocationic organometallopeptides 

      Salvadó, Iria; Gamba, Ilaria; Montenegro García, Javier; Martínez Costas, José Manuel; Brea Floriani, José Manuel; Loza García, María Isabel; Vázquez López, Miguel; Vázquez Sentís, Marco Eugenio (Royal Society of Chemistry, 2016-08-19)
      A series of oligoarginine peptide derivatives containing cyclometallated iridium(III) units display remarkable cytotoxicity, comparable to that of cisplatin. In vitro studies with unilamellar vesicles support a membrane-disrupting ...
    • Merging supramolecular and covalent helical polymers: four helices within a single scaffold 

      Fernández Villar, Zulema; Fernández Rodríguez, Berta; Quiñoá Cabana, Emilio; Freire Iribarne, Félix Manuel (ACS Publications, 2021)
      Supramolecular and covalent polymers share multiple structural effects such as chiral amplification, helical inversion, sergeants and soldiers, or majority rules, among others. These features are related to the axial helical ...
    • Messenger RNA delivery by hydrazone-activated polymers 

      Juanes, Marisa; Creese, Oliver; Fernández Trillo, Francisco; Montenegro García, Javier (Royal Society of Chemistry, 2019)
      The intracellular delivery of DNA and RNA therapeutics requires the assistance of vectors and/or nucleotide modifications to protect the nucleic acids against host nucleases and promote cellular internalization and release. ...
    • Metal-Catalyzed annulations through activation and cleavage of C−H bonds 

      Gulías Costa, Moisés; Mascareñas Cid, José Luis (WILEY-VCH Verlag GmbH, 2016-06-22)
      The exponential increase in the number of catalytic transformations that involve a metal-promoted activation of hitherto considered inert C−H bonds is promoting a fundamental change in the field of synthetic chemistry. ...
    • Metal-catalyzed Cyclizations to Pyran and Oxazine Derivatives 

      Varela Carrete, Jesús Ángel; Saá Rodríguez, Carlos (Thieme, 2016)
      Pyrans are privileged heterocyclic structures found in numerous natural compounds with extraordinary biological activities. The synthesis of these relevant structures has attracted a great deal of attention over the years. ...
    • Metal-catalyzed uncaging of DNA-binding agents in living cells 

      Sánchez López, Mateo Isidro; Penas Tallón, Cristina; Vázquez Sentís, Marco Eugenio; Mascareñas Cid, José Luis (Royal Society of Chemistry, 2014)
      Attachment of alloc protecting groups to the amidine units of fluorogenic DNA-binding bisbenzamidines or to the amino groups of ethidium bromide leads to a significant reduction of their DNA affinity. More importantly, the ...
    • Metal-Dependent DNA Recognition and Cell Internalization of Designed, Basic Peptides 

      Learte Aymamí, Soraya; Curado, Natalia; Rodríguez Villar, Jéssica; Vázquez Sentís, Marco Eugenio; Mascareñas Cid, José Luis (American Chemical Society, 2017)
      A fragment of the DNA basic region (br) of the GCN4 bZIP transcription factor has been modified to include two His residues at designed i and i+4 positions of its N-terminus. The resulting monomeric peptide (brHis2) does ...
    • Methyl 2-diphenylphosphoryloxy-2-azabicyclo[2.2.1]hept-5-ene-3-exocarboxylate 

      Sousa, Carlos A.D.; Vale, M. Luísa C.; Rodríguez Borges, José E.; García Mera, Xerardo Xusto (International Union of Crystallography, 2009)
      In the title compound, C20H20NO4P, the dihedral angle between the phenyl rings is 68.52 (7) . In the crystal structure, the molecules are linked by a weak C—H(arene) interaction along [010] involving the phenyl CH group ...
    • Methyl derivatives of tetracyclic psoralen analogues: antiproliferative activity and interaction with DNA 

      Dalla Via, Lisa; Uriarte Villares, Eugenio; Santana Penín, María Lourdes; Marciani Magno, Sebastiano; Gia, Ornella (Arkat USA Inc, 2004)
      A number of new tetracyclic psoralen derivatives were studied. The fourth ring is constituted by cyclopentane (4, 7 and 9), cyclohexane (11, 15 and 18) or benzene (12, 16 and 20) fused to either 4',5' or 3,4 photoreactive ...
    • Microwave-assisted facile synthesis, anticancer evaluation and docking study of N-((5-(substituted methylene amino)-1,3,4-thiadiazol-2-yl)methyl) benzamide derivatives 

      Tiwari, Shailee V.; Siddiqui, Sumaiya; Seijas Vázquez, Julio Antonio; Vázquez Tato, María del Pilar; Sarkate, Aniket; Lokwani, Deepak K.; Nikalje, Anna Pratima G. (MDPI, 2017)
      In the present work, 12 novel Schiff’s bases containing a thiadiazole scaffold and benzamide groups coupled through appropriate pharmacophore were synthesized. These moieties are associated with important biological ...
    • Microwave-induced covalent functionalization of few-layer graphene with arynes under solvent-free conditions 

      Sulleiro, M. V.; Quiroga Fernández, Sabela; Peña Gil, Diego; Pérez Meirás, María Dolores; Guitián Rivera, Enrique Carlos; Criado Fernández, Alejandro; Prato, Maurizio (Royal Society of Chemistry, 2018)
      A non-conventional modification of exfoliated few-layer graphene (FLG) with different arynes under microwave (MW) irradiation and solvent-free conditions is reported. The described approach allows reaching fast, efficient ...
    • MitoBlue as a tool to analyze the mitochondria-lysosome communication 

      Sánchez López, Mateo Isidro; Vida, Yolanda; Pérez-Inestrosa, Ezequiel; Mascareñas Cid, José Luis; Vázquez Sentís, Marco Eugenio; Sugiura, Ayumu; Martínez Costas, José Manuel (Springer Nature, 2020)
      MitoBlue is a fluorescent bisamidine that can be used to easily monitor the changes in mitochondrial degradation processes in different cells and cellular conditions. MitoBlue staining pattern is exceptional among mitochondrial ...





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