BackBrowsing Artículos by Author "Martín Encinas, Endika"
Now showing items 1-13 of 13
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A Dual-Sensor-Based Screening System for In Vitro Selection of TDP1 Inhibitors
; ; ; ; Palacios Gambra, Francisco Javier
; Alonso Pérez, Concepción Estibaliz ; ; (MDPI, 2021-07-15)
DNA sensors can be used as robust tools for high-throughput drug screening of small molecules with the potential to inhibit specific enzymes. As enzymes work in complex biological pathways, it is important to screen for ... -
Antileishmanial Effect of 1,5- and 1,8-Substituted Fused Naphthyridines
; ; Palacios Gambra, Francisco Javier; ; ; ; ; Alonso Pérez, Concepción Estibaliz ; (MDPI, 2023-12-22)
In the absence of a vaccine, there is a need to find new drugs for the treatment of neglected tropical diseases, such as leishmaniasis, that can overcome the many drawbacks of those currently used. These disadvantages ... -
Dynamic Nucleophilic Aromatic Substitution of Tetrazines
(Wiley, 2021-08-23)A dynamic nucleophilic aromatic substitution of tetrazines (SNTz) is presented herein. It combines all the advantages of dynamic covalent chemistry with the versatility of the tetrazine moiety. Indeed, libraries of compounds ... -
Fused 1,5-Naphthyridines: Synthetic Tools and Applications
; Fuertes Sánchez, María; ; ; Rubiales Alcaine, María Gloria ; Palacios Gambra, Francisco Javier ; Alonso Pérez, Concepción Estibaliz (MDPI, 2020-07-31)
Heterocyclic nitrogen compounds, including fused 1,5-naphthyridines, have versatile applications in the fields of synthetic organic chemistry and play an important role in the field of medicinal chemistry, as many of them ... -
Hydrogen sulphide-triggered theranostic prodrugs based on the dynamic chemistry of tetrazines
Perretti, Marcelle D.; Pérez Pérez, Yaiza; Soler Carracedo, Kevin; Martín Encinas, Endika; Alonso Pérez, Concepción Estibaliz; Scoccia, Jimena; Carrillo Fumero, Romen (Royal Society of Chemistry, 2022)
[EN] Dynamic nucleophilic aromatic substitution of tetrazines (S(N)Tz) has been employed to build theranostic prodrugs that are activated by hydrogen sulfide. H2S is typically found in high concentrations in some kinds of ... -
Naphthyridine Derivatives Induce Programmed Cell Death in Naegleria fowleri
Rizo-Liendo, Aitor; Arberas-Jiménez, Iñigo; Martín Encinas, Endika; Sifaoui, Ines; Reyes-Batlle, María; Chao-Pellicer, Javier; Alonso Pérez, Concepción Estibaliz; Palacios Gambra, Francisco Javier ; Piñero, José E.; Lorenzo-Morales, Jacob (MDPI, 2021-10-01)
Primary amoebic encephalitis (PAM) caused by the opportunistic pathogen Naegleria fowleri is characterized as a rapid and lethal infection of the brain which ends in the death of the patient in more than 90% of the reported ... -
Novel phosphine sulphide gold(I) complexes: topoisomerase I inhibitors and antiproliferative agents
; ; ; ; Rubiales Alcaine, María Gloria; ; Palacios Gambra, Francisco Javier ; Alonso Pérez, Concepción Estibaliz (RSC, 2020-05-20)
This work describes the synthesis of the gold(I) complexes of phosphine sulphides. The formation of these new derivatives has been confirmed by X-ray crystallography. The coordination of gold(I) with the sulphur atom of ... -
Novel topoisomerase I inhibitors. Syntheses and biological evaluation of phosphorus substituted quinoline derivates with antiproliferative activity
Alonso Pérez, Concepción Estibaliz; Fuertes Sánchez, María ; ; ; Rubiales Alcaine, María Gloria ; ; ; Palacios Gambra, Francisco Javier (Elsevier, 2018-02-22)
This work describes the synthesis of 1,2,3,4-tetrahydroquinolinylphosphine oxides, phosphanes and phosphine sulfides as well as that of quinolinylphosphine oxides and phosphine sulfides, which were synthesized in good to ... -
Synthesis of Heterocyclic Fused [1,5]naphthyridines by Intramolecular HDA Reactions
Alonso Pérez, Concepción Estibaliz; Martín Encinas, Endika; Rubiales Alcaine, María Gloria ; Palacios Gambra, Francisco Javier (MDPI, 2019-09-06)
Povarov reaction [1] can be considered as an example of HDA reactions and represents an excellent method for the preparation of nitrogen-containing heterocyclic compounds [2]. When aldimines, derived from aromatic amines ... -
Synthesis of novel antiproliferative hybrid bis-(3-indolyl)methane phosphonate derivatives
; ; Alonso Pérez, Concepción Estibaliz; Martínez de Marigorta Izaga, Edorta ; Rubiales Alcaine, María Gloria ; Vicario Hernando, Javier ; Palacios Gambra, Francisco Javier (Elsevier, 2018-09-15)
An efficient synthetic methodology for the preparation of phosphorus substituted bis-(3-indolyl)methane through a double nucleophilic addition of indole derivatives to an in situ generated α-iminophosphonate is reported. ... -
Synthesis of novel hybrid quinolino[4,3-b][1,5]naphthyridines and quinolino[4,3-b][1,5]naphthyridin-6(5H)-one derivatives and biological evaluation as topoisomerase I inhibitors and antiproliferatives
; ; ; Rubiales Alcaine, María Gloria; ; Palacios Gambra, Francisco Javier ; Alonso Pérez, Concepción Estibaliz (Elsevier, 2020-04-03)
The topoisomerase I enzymatic inhibition of hybrid quinolino [4,3-b] (Siegel et al., 2013; Antony et al., 2003) [1,5]naphthyridines and quinolino [4,3-b] (Siegel et al., 2013; Antony et al., 2003) [1,5]naphthyridin-6(5H)-ones ... -
Synthesis, biological and computational evaluation of novel cyanomethyl vinyl ether derivatives
; Fuertes Sánchez, María; ; ; ; Alonso Pérez, Concepción Estibaliz (Frontiers Media, 2024)
This work explores the biological evaluation of novel cyanomethyl vinyl ether derivatives as antiproliferative agents. Tubulin, crucial to microtubule structure and function, is a target for cancer therapies. In vitro ... -
Synthetic Strategies, Reactivity and Applications of 1,5-Naphthyridines
Fuertes Sánchez, María; Masdeu Margalef, Carme; Martín Encinas, Endika; Selas Lanseros, Asier; Rubiales Alcaine, María Gloria ; Palacios Gambra, Francisco Javier ; Alonso Pérez, Concepción Estibaliz (MDPI, 2020-07-16)
This review covers the synthesis and reactivity of 1,5-naphthyridine derivatives published in the last 18 years. These heterocycles present a significant importance in the field of medicinal chemistry because many of them ...