Listar por autoría "751b57cd-50b0-470a-8b8f-5be1d5cc2ed5"
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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 ... -
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/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 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 ... -
Design, synthesis and antimalarial evaluation of novel thiazole derivatives
Bueno, José María; Carda, Miguel; Crespo, Benigno; Cuñat, Ana Carmen; De Cozar, Cristina; León, María Luisa; Marco, J. Alberto; Roda, Nuria; Sanz-Cervera, Juan F. Elsevier (2016)As part of our medicinal chemistry program’s ongoing search for compounds with antimalarial activity, we prepared a series of thiazole analogs and conducted a SAR study analyzing their in vitro activities against the ... -
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 ... -
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 ... -
Novel multitarget inhibitors with antiangiogenic and immunomodulator properties
Conesa Milián, Laura; Falomir, Eva; Murga, Juan; Carda, Miguel; Marco, J. Alberto Elsevier (2019-03-08)By means of docking studies, seventeen compounds T.1-T17 have been designed and evaluated as multitarget inhibitors of VEGFR-2 and PD-L1 proteins in order to overcome resistance phenomena offered by cancer. All these ... -
Short, Stereoselective Synthesis of the Naturally Occurring Pyrrolidine Radicamine B and a Formal Synthesis of Nectrisine
Ribés Vidal, Celia; Falomir, Eva; Carda, Miguel; Marco, J. Alberto American Chemical Society (2008)A short, stereoselective synthesis of the naturally occurring pyrrolidine radicamine B is reported. Garner′s (R)-aldehyde, prepared from d-serine, was the chiral starting material. The pyrrolidine ring was stereoselectively ... -
Stereoselective syntheses of the glycosidase inhibitors hyacinthacine A2, hyacinthacine A3 and 5-epi-hyacinthacine A3
Ribés Vidal, Celia; Falomir, Eva; Carda, Miguel; Marco, J. Alberto Elsevier (2009)Stereoselective syntheses of the naturally occurring glycosidase inhibitors hyacinthacines A2 and A3 are reported. In the case of hyacinthacine A2, the pyrrolizidine system was created from an acyclic precursor via a double ... -
Stereoselective synthesis of a C1-C18 fragment of amphidinolides G and H
García Fortanet, Jorge; Formentín, Pilar; Diaz-Oltra, Santiago; Murga, Juan; Carda, Miguel; Marco, J. Alberto Elsevier (2013-04)A stereoselective synthesis of a C1–C18 segment of the structure of the cytotoxic macrolides amphidinolides G and H is reported. The target compound was retrosynthetically disconnected into three fragments. In the synthetic ...