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.
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.
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.
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
Publicaciones > Valencia et al
1,10a-Dihydro-1-aza-10a-boraphenanthrene and 6a,7-Dihydro-7-aza-6a-boratetraphene: Two New Fluorescent BN-PAHs.
1. Departamento de Química Orgánica y Química Inorgánica, Instituto de Investigación Química "Andrés M. del Río" (IQAR), Universidad de Alcalá, IRYCIS, Campus Científico-Tecnológico, 28805 Alcalá de Henares, Spain. 2. Departamento de Química Analítica, Química Física e Ingeniería Química, Instituto de Investigación Química "Andrés M. del Río" (IQAR), Universidad de Alcalá, Campus Científico-Tecnológico, 28805 Alcalá de Henares, Spain.
Abstract
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 ϕ(F) = 0.80).
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). |
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.
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. |
Two-photon activated precision molecular photosensitizer targeting mitochondria.
Resumen
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.
Publicaciones > Altarejos et al
Enantioselective Copper-Catalyzed Synthesis of Trifluoromethyl-Cyclopropylboronates.
1. Universidad de Alcalá, Departamento de Química Orgánica y Química Inorgánica,, Alcalá de Henares 28805, Spain. 2. Instituto de Investigación Química Andrés Manuel del Río (IQAR), Universidad de Alcalá, Alcalá de Henares 28805, Spain. 3. Instituto Ramón y Cajal de Investigación Sanitaria (IRYCIS), Madrid 28034, Spain.
Abstract
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.
Publicaciones > Garcia-Marin et al
Tripeptides as Integrin-Linked Kinase Modulating Agents Based on a Protein-Protein Interaction with α-Parvin.
1. Departamento de Química Orgánica y Química Inorgánica, Universidad de Alcalá, Alcalá de Henares 28805, Spain. 2. Instituto Ramón y Cajal de Investigación Sanitaria (IRYCIS), Ctra. Colmenar Viejo, km. 9100, Madrid 28034, Spain. 3. Instituto de Investigación Química Andrés Manuel del Río (IQAR), Universidad de Alcalá, Alcalá de Henares 28805, Spain. 4. Departamento de Biología de Sistemas, Universidad de Alcalá, Alcalá de Henares 28805, Spain. 5. Graphenano Medical Care, S.L, Yecla 30510, Spain.
Abstract
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.
