Listar QUIO_Articles por autoría "a95e0bc1-ed95-46a6-a98b-df4cce8ab165"
Mostrando ítems 1-20 de 68
-
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 ... -
A practical procedure of low valent tin mediated Barbier allylation of aldehydes in wet solvent
Vilanova Gallén, Concepción; Sanchez Peris, Maria; Roldán Gómez, Steven; Dhotare, Bhascar; Carda, Miguel; Chattopadhyay, Angshuman Elsevier (2013-11)Use of aluminium as the reducing metal in spontaneous bimetal redox reaction has been elegantly exploited for allylation/crotylation of aldehydes in wet solvent. Here, low valent tin was prepared in situ by reduction of ... -
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 ... -
Antiplasmodial and Cytotoxic Activity of Piper Piedecuestanum Trel. and Yunck
Mesa Vanegas, Ana Maria; Toro Suaza, Jhon Fredy; Vásquez Cardona, Ana María; Blair Trujillo, Silvia; Peláez Jaramillo, Carlos; Diaz-Oltra, Santiago; Angulo-Pachón, César A.; Carda, Miguel Academic Journals, New York (2018)ackground and Objective: Plasmodium resistance to antimalarial drugs has expanded and in tensified, making new and effective antimalarial drugs urgently. The objective of this work was the in vitro evaluation of ... -
Antiplasmodials soulattrolide derivatives from Calophyllum brasiliense and its mechanism of activity
Mesa Vanegas, Ana Maria; Blair Trujillo, Silvia; Peláez Jaramillo, Carlos; Carda, Miguel Elsevier (2019-03)Parasitic diseases such as malaria, leishmaniasis, trypanosomia-sis, and schistosomiasis are just one of the main causes of diseaseand death in the world today (WHO, 2016). In 2016, 91 countriesreported a total of 216 ... -
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 ... -
Chemical constituents and standardization of Piper piedecuestanum TREL & YUNCK. With antiplasmodial and cytotoxic activity
Mesa Vanegas, Ana Maria; Blair Trujillo, Silvia; Peláez Jaramillo, Carlos; Carda, Miguel Cogent OA (2019)Malaria is a parasitic disease that still prevails in the world and has been widely treated with the use of healing herbs. In this work isolation and extraction strategies have been implemented to get five molecules: ... -
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 ... -
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 ...