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Exploring the Surface of the Ectodomain of the PD-L1 Immune Checkpoint with Small-Molecule Fragments
(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 ...
Enols and Allylic Alcohols as Building Blocks in Synthetic Organic Chemistry. Experimental and Theoretical Studies.
(2022-10-21)
The presen thesis describes computational and experimental studies used to drive the reactivity o allylic and enol subtrates towards new transformations. These synthetic methods give access to a number of organic molecules ...
Triazole-Directed Pd-Catalyzed C(sp2)–H Oxygenation of Arenes and Alkenes
(ACS Publications, 2016-02-24)
Selective Pd-catalyzed C(sp2)–H oxygenation of 4-substituted 1,2,3-triazoles is described. Unlike previous metal-catalyzed C–H functionalization events, which preferentially occur at the activated heterocyclic C–H bond, ...
1, 2, 3 - Triazoles as key frameworks in drug discovery & metal catalysis
(2017-07-07)
La tesis se enmarca dentro de la química de los 1H-1,2,3-triazoles y sus sales de N-alquil-triazolio. El trabajo realizado contempla los siguientes objetivos:1.- Sintetizar y estudiar los 1H-1,2,3-triazoles como plantillas ...
Site-Selective Aqueous C–H Acylation of Tyrosine-Containing Oligopeptides with Aldehydes
(RSC, 2020-10-06)
The development of useful synthetic tools to label amino acids within a peptide framework for the ultimate modification of proteins in a late-stage fashion is a challenging task of utmost importance within chemical biology. ...
Site-Selective Trifluoromethylation Reactions of Oligopeptides
(Wiley, 2020-06-08)
Site-selective chemical modifications that target proteinogenic amino acid residues complement the methods entailing genetic manipulation, thereby allowing straightforward and rapid access to engineered proteins. The ...
Metal-catalyzed C–H functionalization processes upon “click”-triazole assistance
(Wiley, 2018-08-24)
The functionalization of otherwise unreactive C–H bonds holds great promise for reducing the reliance on existing functional groups while improving energy efficiency and atom-economy. One of the most powerful strategies ...
Novel studies on organocatalytic and stoichiometric C-C bond forming reactions
(2019-01-28)
Las diferentes generaciones de organocatalizadores basadas en prolinas no naturales han demostrado ser muy eficientes a la hora de catalizar reacciones de formación de enlaces carbono-carbono como la reacción aldólica y ...
Pd-catalyzed site-selective C(sp(2))-H radical acylation of phenylalanine containing peptides with aldehydes
(Royal Society of Chemistry, 2019-08-07)
The site-selective functionalization of C-H bonds within a peptide framework remains a challenging task of prime synthetic importance. Herein, the first Pd-catalyzed delta-C(sp(2))-H acylation of Phe containing peptides ...
Pd-catalyzed site-selective C(sp2)–H radical acylation of phenylalanine containing peptides with aldehydes
(Royal Society of Chemistry, 2019-10-14)
The site-selective functionalization of C-H bonds within a peptide framework remains a challenging task of prime synthetic importance. Herein, the first Pd-catalyzed delta-C(sp(2))-H acylation of Phe containing peptides ...