Browsing by Author "Del Corte Solaguren-Beascoa, Xabier"
Now showing items 1-14 of 14
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1,2-Dihidrokinolina/hidantoina hibridoen sintesia eta aktibitate zitotoxikoaren ebaluazioa
Pellicer Rivera, Ainara (2023-09-06)Azken urteetan, terapia klasikoen eraginkortasun mugatuaren ondorioz, polifarmakologia izeneko konbinazio terapien inguruko ikerketen kopurua handitu egin dela ikusi da. Arlo honen barruan, hainbat itu terapeutiko modulatzeko ... -
5-Ethoxy-1-(4-methoxyphenyl)-5-methyl-3-phenylimidazolidine-2,4-dione
Del Corte Solaguren-Beascoa, Xabier; López Francés, Adrián ; Martínez de Marigorta Izaga, Edorta ; Palacios Gambra, Francisco Javier ; Vicario Hernando, Javier (MDPI, 2021-05-28)The title compound is a hydantoin derivative that has been synthesized through a three-component reaction of ethyl pyruvate, p-anisidine and phenyl isocyanate. This paper provides a comprehensive spectral dataset for the ... -
A Brønsted Acid-Catalyzed Multicomponent Reaction for the Synthesis of Highly Functionalized γ-Lactam Derivatives
Del Corte Solaguren-Beascoa, Xabier; Martínez de Marigorta Izaga, Edorta ; Palacios Gambra, Francisco Javier ; Vicario Hernando, Javier (MDPI, 2019-08)Bronsted acids catalyze a multicomponent reaction of benzaldehyde with amines and diethyl acetylenedicarboxylate to afford highly functionalized gamma-lactam derivatives. The reaction consists of a Mannich reaction of an ... -
A Multicomponent Protocol for the Synthesis of Highly Functionalized γ-Lactam Derivatives and Their Applications as Antiproliferative Agents
Del Corte Solaguren-Beascoa, Xabier; López Francés, Adrián ; Maestro Burzaco, Aitor; Villate Beitia, Ane Ilia; Sainz Ramos, Myriam; Martínez de Marigorta Izaga, Edorta ; Pedraz Muñoz, José Luis ; Palacios Gambra, Francisco Javier ; Vicario Hernando, Javier (MDPI, 2021-08-09)An efficient synthetic methodology for the preparation of 3-amino 1,5-dihydro-2H-pyrrol-2-ones through a multicomponent reaction of amines, aldehydes, and pyruvate derivatives is reported. In addition, the densely substituted ... -
Asymmetric Synthesis of Tetrasubstituted α-Aminophosphonic Acid Derivatives
Maestro Burzaco, Aitor; Del Corte Solaguren-Beascoa, Xabier; López Francés, Adrián ; Martínez de Marigorta Izaga, Edorta ; Palacios Gambra, Francisco Javier ; Vicario Hernando, Javier (MDPI, 2021-05-27)Due to their structural similarity with natural α-amino acids, α-aminophosphonic acid derivatives are known biologically active molecules. In view of the relevance of tetrasubstituted carbons in nature and medicine and the ... -
Chiral self-recognition in a bispericyclic cyclodimerisation reaction of 1-azadienes
López Francés, Adrián ; Del Corte Solaguren-Beascoa, Xabier; Serna Burgos, Zuriñe ; De los Santos Ruiz, Jesús Manuel ; De Cózar Ruano, Abel; Vicario Hernando, Javier (RSC, 2023-10)Hermaphroditism of molecules: as in nature some species behave as male or female depending on the environment, herein we report a bispericyclic dimerisation of cyclic 1-azadienes where a molecule can behave as either diene ... -
Exploring the Surface of the Ectodomain of the PD-L1 Immune Checkpoint with Small-Molecule Fragments
Kitel, Radoslaw; Rodríguez Rodríguez, Ismael; Del Corte Solaguren-Beascoa, Xabier; Atmaj, Jack; Zarnik, Magdalena; Surmiak, Ewa; Muszak, Damian; Magiera-Mularz, Katarzyna; Popowicz, Grzegorz M.; Holak, Tad A.; Musielak, Bogdan (American Chemical Society, 2022-09-08)Development of small molecules targeting the PD-L1/PD-1 interface is advancing both in industry and academia, but only a few have reached early-stage clinical trials. Here, we take a closer look at the general druggability ... -
Exploring the Synthetic Potential of γ-Lactam Derivatives Obtained from a Multicomponent Reaction—Applications as Antiproliferative Agents
López Francés, Adrián ; Del Corte Solaguren-Beascoa, Xabier; Serna Burgos, Zuriñe ; Martínez de Marigorta Izaga, Edorta ; Palacios Gambra, Francisco Javier ; Vicario Hernando, Javier (MDPI, 2022)[EN] A study on the reactivity of 3-amino α,β-unsaturated γ-lactam derivatives obtained from a multicomponent reaction is presented. Key features of the substrates are the presence of an endocyclic α,β-unsaturated amide ... -
Inmunoterapia: vacunas terapéuticas para tratar el cáncer de páncreas
Ulanga Ganuza, Amaia Ane (2023-09-06)El cáncer de páncreas es una patología que se caracteriza por un crecimiento anómalo de las células endoteliales de los conductos exocrinos del órgano. Actualmente, es uno de los tumores más letales a nivel mundial y pese ... -
Multicomponent Synthesis of Unsaturated γ-Lactam Derivatives. Applications as Antiproliferative Agents through the Bioisosterism Approach: Carbonyl vs. Phosphoryl Group
Del Corte Solaguren-Beascoa, Xabier; López Francés, Adrián ; Villate Beitia, Ane Ilia; Sainz Ramos, Myriam; Martínez de Marigorta Izaga, Edorta ; Palacios Gambra, Francisco Javier ; Alonso Pérez, Concepción Estibaliz ; De los Santos Ruiz, Jesús Manuel ; Pedraz Muñoz, José Luis ; Vicario Hernando, Javier (MDPI, 2022-04-22)We report efficient synthetic methodologies for the preparation of 3-amino and 3-hydroxy 3-pyrrolin-2-ones (unsaturated γ-lactams) through a multicomponent reaction of amines, aldehydes and acetylene or pyruvate derivatives. ... -
Multicomponent synthesis of γ-lactam derivatives and applications as anticancer agents
Del Corte Solaguren-Beascoa, Xabier (2022-10-06)Cancer, the name given to a collection of neoplastic diseases, is the second most important global cause of death. For ages, the treatment of these diseases has been a highly complex process and, although several innovative ... -
Nutlin-3a-aa: Improving the Bioactivity of a p53/MDM2 Interaction Inhibitor by Introducing a Solvent-Exposed Methylene Group
Nietzold, Florian; Rubner, Stefan; Labuzek, Beata; Golik, Przemyslaw; Surmiak, Ewa; Del Corte Solaguren-Beascoa, Xabier; Kitel, Radoslaw; Protzel, Christoph; Reppich-Sacher, Regina; Stichel, Jan; Magiera-Mularz, Katarzyna; Holak, Tad A. A.; Berg, Thorsten (Wiley, 2023-03)Nutlin-3a is a reversible inhibitor of the p53/MDM2 interaction. We have synthesized the derivative Nutlin-3a-aa bearing an additional exocyclic methylene group in the piperazinone moiety. Nutlin-3a-aa is more active than ... -
Synthesis of Tetrasubstituted Phosphorus Analogs of Aspartic Acid as Antiproliferative Agents
Del Corte Solaguren-Beascoa, Xabier; Maestro Burzaco, Aitor; López Francés, Adrián ; Palacios Gambra, Francisco Javier ; Vicario Hernando, Javier (MDPI, 2022-11-18)An efficient general method for the synthesis of a wide family of α-aminophosphonate analogs of aspartic acid bearing tetrasubstituted carbons is reported through an aza-Reformatsky reaction of α-iminophosphonates, generated ... -
Ugi Reaction on α-Phosphorated Ketimines for the Synthesis of Tetrasubstituted α-Aminophosphonates and Their Applications as Antiproliferative Agents
López Francés, Adrián ; Del Corte Solaguren-Beascoa, Xabier; Martínez de Marigorta Izaga, Edorta ; Palacios Gambra, Francisco Javier ; Vicario Hernando, Javier (MDPI, 2021-03-16)An Ugi three-component reaction using preformed α-phosphorated N-tosyl ketimines with different isocyanides in the presence of a carboxylic acid affords tetrasubstituted α-aminophosphonates. Due to the high steric hindrance, ...