Listar QUIO_Articles por autoría "c6ce0057-d1c7-4664-af02-b2c531cdb1a0"
Mostrando ítems 21-40 de 41
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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 ... -
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 ... -
Stereoselective Synthesis of the Cytotoxic 14-Membered Macrolide Aspergillide A
Diaz-Oltra, Santiago; Angulo-Pachón, César A.; Murga, Juan; Carda, Miguel; Marco, J. Alberto American Chemical Society (2010)A stereoselective synthesis of the cytotoxic 14-membered macrolide aspergillide A has been performed. The preparation of a cis-2,6-disubstituted tetrahydropyran ring via stereoselective reduction of an intermediate cyclic ... -
Stereoselective synthesis of the cytotoxic macrolide aspergillide B
Diaz-Oltra, Santiago; Angulo-Pachón, César A.; Kneeteman, María N.; Murga, Juan; Carda, Miguel; Marco, J. Alberto Elsevier (2009)A total, stereoselective synthesis of the cytotoxic macrolide aspergillide B has been performed. A cross metathesis and a C-glycosidation via a Mukaiyama-type aldol reaction were key features of the synthesis. The macrocyclic ... -
Stereoselective synthesis of the naturally occurring 2-pyranone dodoneine
Álvarez Bercedo, Paula; Falomir, Eva; Murga, Juan; Carda, Miguel; Marco, J. Alberto Wiley-VCH (2008-08)The first total synthesis of the naturally occurring dihydropyranone dodoneine is reported. Asymmetric allylations were used for the stereoselective generation of the two stereogenic centers. The pyranone ring was created ... -
Synthesis and biological evaluation as antiangiogenic agents of ureas derived from 3′-aminocombretastatin A-4
Conesa Milián, Laura; Falomir, Eva; Murga, Juan; Carda, Miguel; Marco, J. Alberto Elsevier (2019-01-15)Twenty-six compounds derived from 3′-aminocombretastatin A-4 (AmCA-4) containing a urea fragment mimicking the structure of Sorafenib, have been synthesized and evaluated as antiangiogenic compounds. Antiproliferative ... -
Synthesis and Biological Evaluation As Microtubule-Active Agents of Several Tetrahydrofuran and Spiroacetal Derivatives
Carda, Miguel; Murga, Juan; Angulo-Pachón, César A.; García Pla, Jorge; Diaz-Oltra, Santiago; Marco, J. Alberto; Trigili, Chiara; Redondo Horcajo, Mariano; Díaz, J. Fernando; Barasoain, Isabel Bentham Science (2013)The stereoselective preparation of several molecules containing structural fragments of the tetrahydrofuran and spiroacetal type is described. Their degree of cytotoxicity and their interactions with tubulin have been ... -
Synthesis and Biological Evaluation of a-Tubulin-Binding Pironetin Analogues with Enhanced Lipophilicity
Carda, Miguel; Murga, Juan; Falomir, Eva; Diaz-Oltra, Santiago; García Pla, Jorge; Paños Pérez, Julián; Trigili, Chiara; Díaz, J. Fernando; Barasoain, Isabel; Marco, J. Alberto Wiley-VCH Verlag (2013)The preparation of four new lipophilic analogues of the natural pyrone pironetin is described. The nine-carbon side chain of the latter has been replaced in one analogue by a 4-phenylbutyl chain and in the other three ... -
Synthesis and biological evaluation of carbamates derived from aminocombretastatin A-4 as vascular disrupting agents
Conesa Milián, Laura; Falomir, Eva; Murga, Juan; Carda, Miguel; Meyen, Eef; Liekens, Sandra; Marco, J. Alberto Elsevier (2018-03-10)A series of t wenty-six carbamates derived from aminocombretastatin A- 4 (AmCA-4 ) were syn thesized and evaluated for their capacity to affect cell proliferation, tubulin polymerization, mitotic cell arrest, microtubule ... -
Synthesis and biological evaluation of cyclic derivatives of combretastatin A-4 containing group 14 elements
Blasco, Víctor; Murga, Juan; Falomir, Eva; Carda, Miguel; Royo, Santiago; Cuñat, Ana Carmen; Sanz-Cervera, Juan F.; Marco, J. Alberto Royal Society of Chemistry (2018)Several tricyclic compounds inspired by the structure of combretastatin A-4 and bearing group 14 elements have been synthesized by homocoupling lithiated aryl fragments followed by ring-closing metathesis. These tricyclic ... -
Synthesis and biological evaluation of simplified pironetin analogues with modifications in the side chain and the lactone ring
Roldán Gómez, Steven; Cardona, Adrià; Conesa Milián, Laura; Murga, Juan; Falomir, Eva; Carda, Miguel; Marco, J. Alberto Royal Society of Chemistry (2017)The preparation of several new analogues of the natural dihydropyrone pironetin is described. They differ from the natural product mainly in the nature of the side chain and the lactone ring. Their cytotoxic activity has ... -
Synthesis and biological evaluation of truncated α-tubulin-binding pironetin analogues lacking alkyl pendants in the side chain or the dihydropyrone ring
Paños Pérez, Julián; Diaz-Oltra, Santiago; Sanchez Peris, Maria; García Pla, Jorge; Murga, Juan; Falomir, Eva; Carda, Miguel; Redondo Horcajo, Mariano; Fernando Díaz, J.; Barasoain, Isabel; Alberto Marco, J. Royal Society of Chemistry (2013)The preparation of several new truncated analogues of the natural dihydropyrone pironetin is described. They differ from the natural product mainly in the suppression of some of the alkyl pendants in either the side chain ... -
Synthesis and biological properties of the cytotoxic 14-membered macrolides aspergillide A and B
Diaz-Oltra, Santiago; Angulo-Pachón, César A.; Murga, Juan; Falomir, Eva; Carda, Miguel; Marco, J. Alberto Wiley (2010-11-09)Total, stereoselective syntheses of the naturally occurring, cytotoxic macrolides aspergillide A and B are described. Olefin metatheses and asymmetric allylations were key steps in the synthetic sequences. Cytotoxicity ... -
Synthesis and evaluation of biphenyl derivatives as potential downregulators of VEGF protein secretion and telomerase-related gene expressions
Sanchez Peris, Maria; Falomir, Eva; Murga, Juan; Carda, Miguel; Marco, J. Alberto Elsevier (2016)A group of 47 biphenyl functionalized compounds, prepared by means of Suzuki couplings, has been investigated for their cytotoxicity on two tumoral cell lines (HT-29 and MCF-7) and one non tumoral cell line (HEK-293). ... -
Synthesis of Combretastatin A-4 and 3 0 -Aminocombretastatin A-4 derivatives with Aminoacid Containing Pendants and Study of their Interaction with Tubulin and as Downregulators of the VEGF, hTERT and c-Myc Gene Expression
Agut, Raúl; Falomir, Eva; Murga, Juan; Martín Beltrán, Celia; Gil Edo, Raquel; Pla, Alberto; Carda, Miguel; Marco, J. Alberto MDPI (2020)Natural product combretastatin A-4 (CA-4) and its nitrogenated analogue 3 0 -aminocombretastatin A-4 (AmCA-4) have shown promising antitumor activities. In this study, a range of CA-4 and AmCA-4 derivatives containing ... -
Synthesis of combretastatin A-4 O-alkyl derivatives and evaluation of their cytotoxic, antiangiogenic and antitelomerase activity
Torijano Gutiérrez, Sandra Adela; Diaz-Oltra, Santiago; Falomir, Eva; Murga, Juan; Carda, Miguel; Marco, J. Alberto Elsevier (2013-12)We here report the synthesis and biological evaluation of several combretastatin A-4 derivatives alkylated at the phenol hydroxyl group. Some of these derivatives contain an (E)-arylalkene fragment reminiscent of that ... -
Synthesis of honokiol analogues and evaluation of their modulating action on VEGF protein secretion and telomerase-related gene expressions
Sanchez Peris, Maria; Murga, Juan; Falomir, Eva; Carda, Miguel; Marco, J. Alberto Wiley (2017-04)A group of 36 biphenyl derivatives structurally related to honokiol were synthesized by means of Suzuki coupling reactions. Their cytotoxicities were evaluated and compared to that of honokiol. Some of the compounds were ... -
The atypical dopamine transport inhibitor, JHW 007, prevents amphetamine-induced sensitization and synaptic reorganization within the nucleus accumbens
Murga, Juan; Velázquez Sánchez, Clara; García-Verdugo, Jose Manuel; Canales, Juan José Elsevier (2013)Benztropine (BZT) analogs, a family of agents with high affinity for the dopamine transporter have been postulated as potential treatments in stimulant abuse due to their ability to attenuate a wide range of effects evoked ... -
The Dopamine Uptake Inhibitor 3α-[bis(4′-fluorophenyl)metoxy]-tropane Reduces Cocaine-Induced Early-Gene Expression, Locomotor Activity, and Conditioned Reward
Velázquez Sánchez, Clara; Ferragud, Antonio; Hernández-Rabaza, Vicente; Nácher, Amparo; Merino, Virginia; Carda, Miguel; Murga, Juan; Canales, Juan José Nature Publishing Group (2009)Benztropine (BZT) analogs, a family of high-affinity dopamine transporter ligands, are molecules that exhibit pharmacological and behavioral characteristics predictive of significant therapeutic potential in cocaine ... -
The high affinity dopamine uptake inhibitor, JHW 007, blocks cocaine-induced reward, locomotor stimulation and sensitization
Velázquez Sánchez, Clara; Ferragud, Antonio; Murga, Juan; Carda, Miguel; Canales, Juan José Elsevier (2010)The discovery and evaluation of high affinity dopamine transport inhibitors with low abuse liability is an important step toward the development of efficacious medications for cocaine addiction. We examined in mice the ...