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Molecular basis of the selective binding of MDMA enantiomers to the Alpha4Beta2 nicotinic receptor subtype: synthesis, pharmacological evaluation and mechanistic studies
(Elsevier + French Société de Chimie Thérapeutique, 2014-06)
The α4β2 nicotinic acetylcholine receptor (nAChR) is a molecular target of 3,4-methylenedioxymethamphetamine (MDMA), a synthetic drug also known as ecstasy, and it modulates the MDMA-mediated reinforcing ...
Introducción a la química combinatoria
(Asociación de Químicos e Ingenieros del Instituto Químico de Sarrià, 2002)
Durante los últimos diez años la Química Combinatoria se ha convertido en una técnica usual para el descubrimiento y desarrollo de nuevos productos con actividad biológica. El presente minireview pretende ...
In silico discovery of substituted pyrido[2,3-d]pyrimidines and pentamidine-like compounds with biological activity in myotonic dystrophy models
(Public Library of Science (PLoS), 2017-06)
Myotonic dystrophy type 1 (DM1) is a rare multisystemic disorder associated with an expansion of CUG repeats in mutant DMPK (dystrophia myotonica protein kinase) transcripts; the main effect of these ...
Expanding the Diversity at the C-4 Position of Pyrido[2,3-d]pyrimidin-7(8H)-ones to Achieve Biological Activity against ZAP-70
(MDPI, 2021-12-15)
Pyrido[2,3-d]pyrimidin-7(8H)-ones have attracted widespread interest due to their similarity with nitrogenous bases found in DNA and RNA and their potential applicability as tyrosine kinase inhibitors. ...
Heteroacoplamientos catalizados por paladio
(Asociación de Químicos e Ingenieros del Instituto Químico de Sarrià, 2002)
Durante los diez últimos años la química del paladio se ha aplicado intensamente en síntesis orgánica debido a su versatilidad y a su gran selectividad. En esta breve revisión se muestran las características ...
Activity of the novel BCR kinase inhibitor IQS019 in preclinical models of B-cell non-Hodgkin lymphoma
(BioMed Central, 2017-03)
Background
Pharmacological inhibition of B cell receptor (BCR) signaling has recently emerged as an effective approach in a wide range of B lymphoid neoplasms. However, despite promising clinical activity ...
Deconstructing Markush: Improving the R&D Efficiency Using Library Selection in Early Drug Discovery
(MDPI, 2022)
Most of the product patents claim a large number of compounds based on a Markush structure. However, the identification and optimization of new principal active ingredients is frequently driven by a ...
Porficenos para la fotoquimioterapia del cáncer y otras aplicaciones biomédicas
(Asociación de Químicos e Ingenieros del Instituto Químico de Sarrià, 2002)
La terapia fotodinámica (PDT) o fotoquimioterapia del cáncer es una modalidad terapéutica que consiste en la aplicación de compuestos fotosensibilizadores que se acumulan preferentemente en tejidos ...
Structural implications of the DFD-in domain in computer-aided molecular design of MAP kinase interacting kinase 2 inhibitors
(Asociación de Químicos e Ingenieros del Instituto Químico de Sarrià, 2017-04)
Protein translation is a key process on cell development and proliferation that is often deregulated in cancer. MAP kinase interacting kinases 1 and 2 (Mnk1/2) play a pivotal role in regulating the ...
Autocatalytic photoinduced oxidative dehydrogenation of pyrido[2,3-d]pyrimidin-7(8H)-ones: synthesis of C5–C6 unsaturated systems with concomitant formation of a long-lived radical
(American Chemical Society, 2024-01-07)
5,6-Dihydropyrido[2,3-d]pyrimidin-7(8H)-ones are readily accessed by a variety of methods and are a good scaffold for the development of biologically active compounds. However, they are very reluctant ...