Archivo de la categoría: Noticias

Noticias

Conferencia Prof. Francisco Corzana, 15.12.21

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Conferencia Prof. Francisco Corzana

El Prof. Francisco Corzana de la Universidad de La Rioja impartirá una conferencia titulada Exploiting the use of unnatural glycopeptide based antigens to detect and fight cancer en la Sala de Grados, Edificio de Farmacia de la UAH el día 15 de diciembre a las 12.00.

conferencia Corzana

(fotografías 1, 2)

Noticias

Conferencia Prof. Álvaro Somoza, 03.12.21

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Conferencia Prof. Álvaro Somoza

El Prof. Álvaro Somoza del Instituto IMDEA Nanociencia impartirá una conferencia titulada Smart Nanomedicines Against Cancer en la Sala de Grados, Edificio de Farmacia de la UAH el día 3 de diciembre a las 12.00.

conferencia Somoza

(fotografías 1, 2)

Noticias

Organización XVII SIJ-RSEQ

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Organización XVII SIJ-RSEQ

Varios componentes del grupo se han encargado de organizar el XVII Simposio de Investigadores Jóvenes de la RSEQ, celebrado en Alcalá de Henares del 23 al 26 de noviembre.

XVII Simposio de Investigadores Jóvenes de la RSEQ

Además, ha contribuido con diversas contribuciones:

– Oral:
· Synthesis of seven- and eight-membered rings by Brønsted acid-catalyzed cyclization of biphenyl embedded trienynes
Jaime Tostado Sánchez, Juan J. Vaquero, Manuel A. Fernández-Rodríguez

– Flash:
· Enantio- and diastereoselective cyclopropanation of trans-alkenylboronates: Synthesis of versatile (trifluoromethyl)cyclopropylboronates
Julia Altarejos, David Sucunza, Juan José Vaquero, Javier Carreras

– Poster:
· Synthesis of a series of novel bicyclic amino acids
Álvaro González, Francisco José Torrero, José Luis Aceña, Juan José Vaquero

· Metal-free straightforward synthesis of boron-functionalized indenes and fulvenes by borylative cyclization
Ester Sans Panadés, Patricia García-García, Juan J. Vaquero, Cintia Virumbrales, Roberto Sanz, Manuel A. Fernández-Rodríguez

· SYNTHESIS OF PEPTIDE NUCLEIC ACIDS (PNAs) FOR THE TREATMENT OF CHRONIC KIDNEY DISEASE
Francisco Maqueda Zelaya, Verónica Miguel, José Luis Aceña, Santiago Lamas, Juan José Vaquero

· Synthesis of 4-membered rings fused lactams by gold(I) catalyzed
cyclization of alkynylcyclobutanamides
Guillermo G. Otárola, María Soledad Garre, Estíbaliz Merino, David Sucunza, Juan J. Vaquero, Patricia García-García

· Regioselective Ir-Catalyzed C−H Borylation of 4a,8a-Dihydro-4a-Aza-8a-Boranaphthalene
Isabel Valencia, Patricia García, David Sucunza, Juan J. Vaquero

· DEVELOPMENT OF A SYNTHETIC ROUTE TO LAETEVIRENOL A
Lucía Sánchez-Jiménez, Ana Milián, Jaime Tostado, Juan J. Vaquero, Patricia García-García, Manuel A. Fernández-Rodríguez

· Kinetic resolution in transannular Morita-Baylis-Hillman reaction:
approach to the synthesis of guaiane-type sesquiterpenes
Rubén Manzano, Raquel Mato, Efraím Reyes, Liher Prieto, Uxue Uria, Luisa Carrillo, Jose L. Vicario

· Electrochemical synthesis of aryl iodides from arylhydrazines
Clara Mañas Hernández, Guillermo Otárola, Estíbaliz Merino, Noemi Salardón, Belén Batanero

Noticias

Nuevo artículo, J. Org. Chem. 11.21

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1,10a-Dihydro-1-aza-10a-boraphenanthrene and 6a,7-Dihydro-7-aza-6a-boratetraphene: Two New Fluorescent BN-PAHs

Isabel Valencia, Patricia García-García, David Sucunza*, Francisco Mendicuti, Juan J. Vaquero*

J. Org. Chem. 2021, 86, 23, 16259–16267
DOI: 10.1021/acs.joc.1c01095

Previously unknown 1,10a-dihydro-1-aza-10a-boraphenanthrene and 6a,7-dihydro-7-aza-6a-boratetraphene have been efficiently synthesized. Bromination of these BN-PAHs proceeds with complete regioselectivity, resulting in the formation of different substituted derivatives via cross-coupling reactions. These compounds exhibit rather high fluorescence quantum yields (up to ϕF = 0.80).
Noticias

Conferencia Dr. Antonio Leyva, 16.11.21

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Conferencia Dr. Antonio Leyva

El Dr. Antonio Leyva del Instituto de Tecnología Química (CSIC-UPV) impartirá una conferencia titulada Highly Efficient Catalysts for Organic Synthesis en la Sala de Grados, Edificio de Farmacia de la UAH el día 16 de noviembre a las 13.00.

conferencia Leyva

(fotografías: 1, 2)

Noticias

Nuevo artículo, Eur. J. Med. Chem. 10.21

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Pyridazino-pyrrolo-quinoxalinium salts as highly potent and selective leishmanicidal agents targeting trypanothione reductase

Héctor de Lucio, Javier García-Marín, Patricia Sánchez-Alonso, Juan Carlos García-Soriano, Miguel Ángel Toro, Juan J Vaquero, Federico Gago, Ramón Alajarín, Antonio Jiménez-Ruiz

Eur. J. Med. Chem. , 2021
DOI: 10.1016/j.ejmech.2021.113915

Fifteen pyridazino-pyrrolo-quinoxalinium salts were synthesized and tested for their antiprotozoal activity against Leishmania infantum amastigotes. Eleven of them turned out to be leishmanicidal, with EC(50) values in the nanomolar range, and displayed low toxicity against the human THP-1 cell line. Selectivity indices for these compounds range from 10 to more than 1000. Compounds 3b and 3f behave as potent inhibitors of the oxidoreductase activity of the essential enzyme trypanothione disulfide reductase (TryR). Interestingly, binding of 3f is not affected by high trypanothione concentrations, as revealed by the noncompetitive pattern of inhibition observed when tested in the presence of increasing concentrations of this substrate. Furthermore, when analyzed at varying NADPH concentrations, the characteristic pattern of hyperbolic uncompetitive inhibition supports the view that binding of NADPH to TryR is a prerequisite for inhibitor-protein association. Similar to other TryR uncompetitive inhibitors for NADPH, 3f is responsible for TryR-dependent reduction of cytochrome c in a reaction that is typically inhibited by superoxide dismutase.
Noticias

Nuevo artículo, Commun. Chem. 10.21

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Two-photon activated precision molecular photosensitizer targeting mitochondria

Inês F. A. Mariz, Sandra N. Pinto, Ana M. Santiago, José M. G. Martinho, Javier Recio, Juan J. Vaquero, Ana M. Cuadro,* Ermelinda Maçôas*

Commun Chem 2021, 4, 142
DOI: 10.1038/s42004-021-00581-4

Mitochondria metabolism is an emergent target for the development of novel anticancer agents. It is amply recognized that strategies that allow for modulation of mitochondrial function in specific cell populations need to be developed for the therapeutic potential of mitochondria-targeting agents to become a reality in the clinic. In this work, we report dipolar and quadrupolar quinolizinium and benzimidazolium cations that show mitochondria targeting ability and localized light-induced mitochondria damage in live animal cells. Some of the dyes induce a very efficient disruption of mitochondrial potential and subsequent cell death under two-photon excitation in the Near-infrared (NIR) opening up possible applications of azonia/azolium aromatic heterocycles as precision photosensitizers. The dipolar compounds could be excited in the NIR due to a high two-photon brightness while exhibiting emission in the red part of the visible spectra (600–700 nm). Interaction with the mitochondria leads to an unexpected blue-shift of the emission of the far-red emitting compounds, which we assign to emission from the locally excited state. Interaction and possibly aggregation at the mitochondria prevents access to the intramolecular charge transfer state responsible for far-red emission.
Noticias

Participación RSEQ Symposium 2021

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Participación RSEQ Symposium 2021

 

El grupo ha contribuido en el primer RSEQ Symposium 2021, organizado entre el 27-30 de septiembre, con diversas contribuciones:

– Oral:
· Enantioselective synthesis of 2,3-substituted cyclopropylboronates
Julia Altarejos, David Sucunza, Juan J. Vaquero, Javier Carreras

– Póster:
· Visible light-mediated enantioselective aminoarylation of alkenes: streamlined access to ?,?-diarylethylamines
Estíbaliz Merino, Cedric Hervieu, Mariia Kirillova,Yawen Hu, Cristina Nevado

· Metal-Free Temperature-controlled Regiodivergent Borylative Cyclization of enynes: a Boron-migration Promoted Skeletal Rearrangement
Ana Milián, Manuel A. Fernández-Rodriguez, Patricia García-García, Estíbaliz Merino, Juan J. Vaquero

· Functionalization of 4a,8a-Dihydro-4a-Aza-8a-Boranaphthalene via Regioselective Iridium-Catalyzed C−H Borylation
Patricia García-García, David Sucunza, Juan J. Vaquero, Isabel Valencia

Noticias

Nuevo artículo, Org. Lett. 07.21

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Enantioselective Copper-Catalyzed Synthesis of Trifluoromethyl-Cyclopropylboronates

Julia Altarejos, David Sucunza, Juan J. Vaquero, and Javier Carreras*

Org. Lett., 2021, ASAP
DOI: 10.1021/acs.orglett.1c02420

A copper-catalyzed enantioselective cyclopropanation involving trifluorodiazoethane in the presence of alkenyl boronates has been developed. This transformation enables the preparation of 2-substituted-3-(trifluoromethyl)cyclopropylboronates with high levels of stereocontrol. The products are valuable synthetic intermediates by transformation of the boronate group. This methodology can be applied to the synthesis of novel trifluoromethylated analogues of trans-2-arylcyclopropylamines, which are prevalent motifs in biologically active compounds.
Noticias

Nuevo artículo, ACS Med. Chem. Lett. 07.21

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Tripeptides as Integrin-Linked Kinase Modulating Agents Based on a Protein–Protein Interaction with α-Parvin

Javier Garcia-Marin,* Mercedes Griera-Merino, Alejandra Matamoros-Recio, Sergio de Frutos, Manuel Rodríguez-Puyol, Ramón Alajarín, Juan J. Vaquero,* Diego Rodríguez-Puyol*

ACS Med. Chem. Lett. , 2021, In Press
DOI: 10.1021/acsmedchemlett.1c00183

Integrin-linked kinase (ILK) has emerged as a controversial pseudokinase protein that plays a crucial role in the signaling process initiated by integrin-mediated signaling. However, ILK also exhibits a scaffolding protein function inside cells, controlling cytoskeletal dynamics, and has been related to non-neoplastic diseases such as chronic kidney disease (CKD). Although this protein always acts as a heterotrimeric complex bound to PINCH and parvin adaptor proteins, the role of parvin proteins is currently not well understood. Using in silico approaches for the design, we have generated and prepared a set of new tripeptides mimicking an α-parvin segment. These derivatives exhibit activity in phenotypic assays in an ILK-dependent manner without altering kinase activity, thus allowing the generation of new chemical probes and drug candidates with interesting ILK-modulating activities.