Listar QUIO_Articles por autoría "c6ce0057-d1c7-4664-af02-b2c531cdb1a0"
Mostrando ítems 1-20 de 41
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A dopamine transport inhibitor with markedly low abuse liability suppresses cocaine self-administration in the rat
Ferragud, Antonio; Velázquez Sánchez, Clara; Hernández-Rabaza, Vicente; Nácher, Amparo; Merino, Virginia; Carda, Miguel; Murga, Juan; Canales, Juan José Springer-Verlag (2009)RATIONALE N-substituted benztropine analogs are potent dopamine uptake inhibitors that display pharmacokinetic/dynamic properties consistent with the profile of a substitute medication for cocaine addiction. OBJECTIVES The ... -
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 ... -
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 ... -
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 ... -
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 ... -
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 ... -
Inhibitory effect of cytotoxic nitrogen-containing heterocyclic stilbene analogues on VEGF protein secretion and VEGF, hTERT and c-Myc gene expression
Martí-Centelles, Rosa; Murga, Juan; Falomir, Eva; Carda, Miguel; Marco, J. Alberto The Royal Society of Chemistry (2015)A group of 21 nitrogen-containing heterocyclic stilbene derivatives, prepared by means of Heck coupling reactions, has been investigated for their cytotoxicity as well as their ability to inhibit the production of the ... -
Inhibitory effect of cytotoxic stilbenes related to resveratrol on the expression of the VEGF, hTERT and c-Myc genes
Martí-Centelles, Rosa; Falomir, Eva; Murga, Juan; Carda, Miguel; Marco, J. Alberto Elsevier (2015)A group of thirty-nine stilbene derivatives, prepared by means of Heck coupling reactions, has been investigated for their cytotoxicity, as well as for their ability to inhibit the production of the vascular endothelial ... -
Inhibitory effect of pironetin analogue/colchicine hybrids on the expression of the VEGF, hTERT and c-Myc genes
Vilanova Gallén, Concepción; Diaz-Oltra, Santiago; Murga, Juan; Falomir, Eva; Carda, Miguel; Marco, J. Alberto Elsevier (2015-08)A small group of hybrid molecules composed of a colchicine moiety and a pironetin analogue fragment have been investigated for their ability to inhibit the expression of the VEGF, hTERT and c-Myc genes. The VEGF gene is ... -
Interactions of long-chain homologues of colchicine with tubulin
Marzo Mas, Ana; Barbier, Pascale; Breuzard, Gilles; Allegro, Diane; Falomir, Eva; Murga, Juan; Carda, Miguel; Peyrot, Vincent; Marco, J. Alberto Elsevier (2017-01)Several colchicine analogues in which the N-acetyl residue has been replaced by aliphatic, straight-chain acyl moieties, have been synthesized. These compounds show high cytotoxic activity at the nanomolar level against ... -
Lung tumorspheres as a drug screening platform against cancer stem cells
Herreros Pomares, Alejandro; Amado, H.; Calabuig, Silvia; Escorihuela, Eva; Murga, Juan; Torres, Susana; Durendez-Saez, Elena; Zhang, F.; Blasco, Ana; Navarro, A.; Sampedro, C.; Jantus Lewintre, Eloisa; Camps, C. Oxford University Press (OUP) (2019-04)Treatment resistance and metastasis are linked to cancer stem cells (CSCs). This population represents a promising target, but remains unexplored in lung cancer. The main objective of this study was to characterize lung ... -
N-alpha-Aminoacyl Colchicines as Promising Anticancer Agents
Marzo Mas, Ana; Conesa Milián, Laura; Noppen, Sam; Liekens, Sandra; Falomir, Eva; Murga, Juan; Carda, Miguel; Marco, J. Alberto Bentham Science Publishers (2020-12-29)Background: In the last years, many efforts have been made to find colchicine derivatives with reduced toxicity. Additionally, the deregulation of amino acid uptake by cancer cells provides an opportunity to improve ...