Listar QUIO_Articles por autoría "50ebe758-4a00-4081-a730-b658c85c91a9"
Mostrando ítems 1-20 de 53
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A formal, stereoselective synthesis of the natural tetrahydropyran derivative ophiocerin D
Paños Pérez, Julián; Murga, Juan; Falomir, Eva; Carda, Miguel; Marco, J. Alberto Elsevier (2010)A short, formal stereoselective synthesis of the naturally occurring tetrahydropyran derivative ophiocerin D is reported. The four stereocenters of the molecule were created with the aid of two Sharpless asymmetric ... -
Aldol Reactions between L-Erythrulose Derivatives and Chiral α-Amino and α -Fluoro Aldehydes: Competition between Felkin–Anh and Cornforth Transition States
Diaz-Oltra, Santiago; Carda, Miguel; Murga, Juan; Falomir, Eva; Marco, J. Alberto Wiley-Blackwell (2008)Both matched and mismatched diastereoselection have been observed in aldol reactions of a boron enolate of a protected l-erythrulose derivative with several chiral α-fluoro and α-Amino aldehydes. Strict adherence to the ... -
Aryl azoles based scaffolds for disrupting tumor microenvironment
Pla López, Alberto; Martinez-Colomina, Paula; Cañada-García, Laura; Fuertes-Monge, Laura; Orellana-Palacios, Jose C.; Valderrama-Martínez, Alejandro; Pérez Sosa, Marikena; Carda, Miguel; Falomir, Eva Elsevier (2023-11-15)Thirty-nine aryl azoles, thirteen triazoles and twenty-seven tetrazoles, have been synthetized and biologically evaluated to determine their activity as tumor microenvironment disruptors. Antiproliferative studies have ... -
Aryl urea based scaffolds for multitarget drug discovery in anticancer immunotherapies
Martín Beltrán, Celia; Gil-Edo, Raquel; Hernández Ribelles, Germán; Agut, Raúl; Marí Mezquita, Pilar; Carda, Miguel; Falomir, Eva MDPI (2021-04-06)Twenty-one styryl and phenethyl aryl ureas have been synthetized and biologically evaluated as multitarget inhibitors of Vascular endothelial growth factor receptor-2 VEGFR-2 and programmed death-ligand-1 (PD-L1) proteins ... -
Arylpyridines, arylpyrimidines and related compounds as potential modulator agents of the VEGF, hTERT and c-Myc oncogenes
Martín Beltrán, Celia; Sanchez Peris, Maria; Conesa Milián, Laura; Falomir, Eva; Murga, Juan; Carda, Miguel; Alberto Marco, J. Elsevier (2019-03-01)Twenty-four derivatives structurally related to honokiol have been synthesized and biologically evaluated. IC50 values were determined towards the HT-29, MCF-7 and HEK-293 cell lines. Some of these derivatives exhibited ... -
Arylureas derived from colchicine: Enhancement of colchicine oncogene downregulation activity
Blasco, Víctor; Cuñat, Ana Carmen; Sanz-Cervera, Juan F.; Marco, J. Alberto; Falomir, Eva; Murga, Juan; Carda, Miguel Elsevier (2018-04-25)Our efforts to get therapeutically useful colchicine derivatives for the treatment of cancer have led us to synthetize and biologically evaluate twenty-seven N,N′-disubstituted ureas containing a colchicine moiety and an ... -
Convergent, stereoselective syntheses of the glycosidase inhibitors broussonetines C, O and P
Ribés Vidal, Celia; Falomir, Eva; Murga, Juan; Carda, Miguel; Marco, J. Alberto Elsevier (2009)The first syntheses of the polyhydroxylated alkaloids (iminosugars) broussonetines O and P, glycosidase inhibitors of the pyrrolidine class, have been performed in a convergent, stereocontrolled way from d-serine as the ... -
Convergent, stereoselective syntheses of the glycosidase inhibitors broussonetines D and M
Ribés Vidal, Celia; Falomir, Eva; Murga, Juan; Carda, Miguel; Marco, J. Alberto Royal Society of Chemistry (2011-06-03)The first syntheses of the polyhydroxylated alkaloids (iminosugars) broussonetines D and M glycosidase inhibitors of the pyrrolidine class, have been performed in a convergent, stereocontrolled way from D-serine as the ... -
Cytotoxic, antiangiogenic and antitelomerase activity of glucosyl- and acyl- resveratrol prodrugs and resveratrol sulfate metabolites
Falomir, Eva; Lucas, Ricardo; Peñalver, Pablo; Martí-Centelles, Rosa; Dupont, Alexia; Zafra Gómez, Alberto; Carda, Miguel; Morales, Juan C. (2016-06)Resveratrol (RES) is a natural polyphenol with relevant and varied biological activity. However, its low bioavailability and rapid metabolism to its glucuronate and sulfate conjugates has opened a debate on the mechanisms ... -
Design and Synthesis of Pironetin Analogue/Colchicine Hybrids and Study of Their Cytotoxic Activity and Mechanisms of Interaction with Tubulin
Vilanova Gallén, Concepción; Diaz-Oltra, Santiago; Murga, Juan; Falomir, Eva; Carda, Miguel; Redondo Horcajo, Mariano; Fernando Díaz, J.; Barasoain, Isabel; Alberto Marco, J. American Chemical Society (2014-11)We here report the synthesis of a series of 12 hybrid molecules composed of a colchicine moiety and a pironetin analogue fragment. The two fragments are connected through an ester–amide spacer of variable length. The ... -
Design and Synthesis of Pironetin Analogue/Combretastatin A-4 Hybrids and Evaluation of Their Cytotoxic Activity
Torijano Gutiérrez, Sandra Adela; Vilanova Gallén, Concepción; Diaz-Oltra, Santiago; Murga, Juan; Falomir, Eva; Carda, Miguel; Marco, J. Alberto Wiley Online Library (2014)We describe the preparation of a series of hybrid molecules containing a combretastatin A-4 moiety and a pironetin analogue fragment linked by an ester spacer of variable length. The cytotoxic activities of these compounds ... -
Design and synthesis of pironetin analogue/combretastatin A-4 hybrids containing a 1,2,3-triazole ring and evaluation of their cytotoxic activity
Vilanova Gallén, Concepción; Torijano Gutiérrez, Sandra Adela; Diaz-Oltra, Santiago; Murga, Juan; Falomir, Eva; Carda, Miguel; Alberto Marco, J. Elsevier (2014)We here describe the preparation of a series of hybrid molecules containing a combretastatin A-4 moiety and a pironetin analogue fragment connected through a spacer of variable length which includes a 1,2,3-triazole ring. ... -
Design and synthesis of pironetin analogues with simplified structure and study of their interactions with microtubules
Marco, J. Alberto; García Pla, Jorge; Carda, Miguel; Murga, Juan; Falomir, Eva; Trigili, Chiara; Notararigo, Sara; Díaz, J. Fernando; Barasoain, Isabel Elsevier (2011-05)The preparation of a series of pironetin analogues with simplified structure is described. Their cytotoxic activity and their interactions with tubulin have been investigated. It has been found that, while less active than ... -
Double diastereoselection in anti aldol reactions mediated by dicyclohexylchloroborane between an L-erythrulose derivative and chiral aldehydes
Diaz-Oltra, Santiago; Ruiz, Purificación; Falomir, Eva; Murga, Juan; Carda, Miguel; Marco, J. Alberto Royal Society of Chemistry (2012)Anti aldol reactions of an L-erythrulose derivative with several α-chiral aldehydes mediated by dicyclohexylboron chloride are examined. Good yields and stereoselectivities are observed. The results are best explained ... -
Effect of Hyaluronic Acid on the Self-Assembly of a Dipeptide-Based Supramolecular Gel
Giménez Hernández, Bárbara; Falomir, Eva; Escuder, Beatriu Wiley (2023-10-02)The combination of polymers and low molecular weight (LMW) compounds is a powerful approach to prepare new supramolecular materials. Here we prepare two-component hydrogels made by a well-known and biologically active ... -
Effects of Curcuminoid Pyrazoles on Cancer Cells and on the Expression of Telomerase Related Genes
Martí-Centelles, Rosa; Falomir, Eva; Carda, Miguel; Nieto, Carla I.; Cornago, M. Pilar; Claramunt, Rosa M. Wiley (2016-07)A group of 13 curcuminoid pyrazoles was investigated for their cytotoxicity on three tumoral cell lines (HT-29, MCF-7, and HeLa) and one non-tumoral human cell line (HEK-293). The values obtained were compared with those ... -
Effects on tubulin polymerization and down-regulation of c-Myc, hTERT and VEGF genes by colchicine haloacetyl and haloaroyl derivatives
Marzo Mas, Ana; Falomir, Eva; Murga, Juan; Carda, Miguel; Marco, J. Alberto Elsevier (2018-04-25)Several colchicine analogues in which the N-acetyl residue has been replaced by haloacetyl, cyclohexylacetyl, phenylacetyl and various aroyl moieties have been synthesized. The cytotoxic activities of the synthesized ... -
Exploring BenzylethoxyAryl Urea Scaffolds for Multitarget Immunomodulation Therapies
Gil-Edo, Raquel; Hernández Ribelles, Germán; Royo, Santiago; Thawait, Natasha; Serrels, Alan; Carda, Miguel; Falomir, Eva MDPI (2023-05-11)Thirteen benzylethoxyaryl ureas have been synthesized and biologically evaluated as multitarget inhibitors of VEGFR-2 and PD-L1 proteins to overcome resistance phenomena offered by cancer. The antiproliferative activity ... -
Imidazole and Imidazolium antibacterial drugs derived from amino acids
Valls Ten, Adriana; Andreu Olaria, Jose Juan; Luis, Santiago V.; Falomir, Eva; Atrián-Blasco, Elena; Mitchell, Scott George; Altava, Belen MDPI (2020-12-21)The antibacterial activity of imidazole and imidazolium salts is highly dependent upon their lipophilicity, which can be tuned through the introduction of different hydrophobic substituents on the nitrogen atoms of the ... -
Inhibition of VEGF Expression in Cancer Cells and Endothelial Cell Differentiation by Synthetic Stilbene Derivatives
Martí-Centelles, Rosa; Cejudo Marín, Rocío; Falomir, Eva; Murga, Juan; Carda, Miguel; Marco, J. Alberto Elsevier (2013-06-01)We here report the synthesis of several stilbene derivatives. They show a measurable inhibitory effect on angiogenesis, some of them to a higher degree than resveratrol. Test methods included cell proliferation and tube ...