Results 71 to 80 of about 9,957 (210)

Synthetic Cathepsin B Sensitive Adjuvant‐Peptide Conjugates to Target Intracellular Toll‐Like Receptors 7 and 8

ChemistryEurope, EarlyView.
Cathepsin B‐sensitive peptide–adjuvant conjugates are designed, synthesized, and evaluated to deliver an antigenic peptid and an adjuvant targeting Toll‐like receptors 7 and 8 (TLR7/8) to antigen presenting cells. The adjuvant is released by cathepsin B resulting in antigen presentation and TLR mediated T cell activation.
Marjolein M. E. Isendoorn, Giulia Castello, Nico J. Meeuwenoord, Martijn Verdoes, Jeroen D. C. Codée, Ferry Ossendorp, Dmitri V. Filippov   +6 more
wiley   +1 more source

Dinuclear thiazolylidene copper complex as highly active catalyst for azid–alkyne cycloadditions

Beilstein Journal of Organic Chemistry, 2016
A dinuclear N-heterocyclic carbene (NHC) copper complex efficiently catalyzes azide–alkyne cycloaddition (CuAAC) “click” reactions. The ancillary ligand comprises two 4,5-dimethyl-1,3-thiazol-2-ylidene units and an ethylene linker.
Anne L. Schöffler, Ata Makarem, Frank Rominger, Bernd F. Straub   +3 more
doaj   +1 more source

Synthesis of Tris-Heterocycles via a Cascade IMCR/Aza Diels-Alder + CuAAC Strategy

Frontiers in Chemistry, 2019
6-Triazolylmethyl-pyrrolo[3,4-b]pyridin-5-one tris-heterocycles were synthesized in 43–57% overall yields. The two-stage synthesis involved a cascade process (Ugi-3CR/aza Diels-Alder/N-acylation/aromatization) followed by a copper-assisted alkyne-azide ...
Manuel A. Rentería-Gómez, A. Islas‐Jácome, S. Pharande, D. Vosburg, Rocío Gámez‐Montaño   +4 more
semanticscholar   +1 more source

Synthesis and Glycosidase Inhibition Studies of Novel Exoglycals Targeting GH3 Family Enzymes: Insights from Comparative Analysis with Macrolide Antibiotics

Chemistry – A European Journal, EarlyView.
A series of structurally diverse exoglycals was synthesized using a modified Julia‐olefination approach from sugar‐derived precursors. These glycosidase transition‐state mimics were further diversified via CuAAC chemistry to yield triazole‐conjugated analogues.
Elisa Ospanow, Oscar L. Alferez, David L. Jakeman   +2 more
wiley   +1 more source

Synthetic Strategies for Activity‐Based Probes to Decode Ubiquitin‐Like Modifiers

Chemistry – A European Journal, EarlyView.
ABSTRACT Ubiquitin‐like proteins (Ubls) such as SUMO, NEDD8, ISG15, URM1, UFM1, FAT10, ATG8/ATG12, and FUBI are essential regulators of cellular homeostasis, controlling processes from protein stability and trafficking to immune signaling and autophagy.
Saibal Chanda, Alan Pham, SreeNidhi Karnati, Natalia Soto Rodriguez, Alyssa Toner, Wenshe Ray Liu   +5 more
wiley   +1 more source

Heterogeneous catalysis for azide-alkyne bioconjugation in solution via spin column: Attachment of dyes and saccharides to peptides and DNA

BioTechniques, 2015
Copper-catalyzed azide-alkyne cycloaddition (CuAAC) “click” chemistry is widely used and has demonstrated particular utility for bio-orthogonal conjugation reactions.
Jeremy Kallick, Sarah Harris, Andrew K. Udit, Michael G. Hill   +3 more
doaj   +1 more source

Dual Ligand‐Enabled Nondirected C─H Olefination of (Hetero)Arenes for the Synthesis of Clickable Derivatives

Chemistry – A European Journal, EarlyView.
We report an efficient method for late‐stage installation of “clickable” alkyne groups into diverse (hetero)arenes. Using a dual‐ligand palladium catalyst that combines an NASA ligand with an N‐heterocycle, an acrylate unit bearing a terminal alkyne can be introduced via nondirected C─H activation.
Tommaso Braga, Maria Hergert, Manuel van Gemmeren   +2 more
wiley   +1 more source

Synthesis of a novel resorcin[4]arene–glucose conjugate and its catalysis of the CuAAC reaction for the synthesis of 1,4-disubstituted 1,2,3-triazoles in water

RSC Advances, 2019
The Cu(i)-catalyzed azide–alkyne cycloaddition (CuAAC) in aqueous media using resorcin[4]arene glycoconjugate (RG) is reported. The eight β-d-glucopyranoside moieties constructed on the resorcin[4]arene upper rim provide a pseudo-saccharide cavity that ...
A. Husain, K. Bisht
semanticscholar   +1 more source

A Bifunctional Small Molecule Degrader of the Long Noncoding RNA MALAT1 Triplex

Chemistry – A European Journal, EarlyView.
Targeting disease‐linked RNAs with small molecules is often limited by the modest impact of binding RNA structure alone. Here, we present a first‐in‐class bifunctional molecule that degrades the oncogenic lncRNA MALAT‐1 by inducing proximity between the RNA and a cleaving warhead.
Christian A. T. Brega, Benjamin A. Craig, Sigitas Mikutis, Rupert S. J. Proctor, Yuliia Vyborna, Galway Ivey, Maria Eleftheriou, Kostas Tzelepis, Mo Yang, Shaifaly Parmar, Javier Bonet‐Aleta, John S. Schneekloth Jr., Gonçalo J. L. Bernardes   +12 more
wiley   +1 more source

One-Pot Synthesis of Imidazo[1,2-a]pyridines via Groebke–Blackburn–Bienaymé Reaction and CuAAC Assisted by MW

Chemistry Proceedings
Bis-heterocyclic compounds containing imidazo[1,2-a]pyridines (IMPs) are privileged heterocyclic drug scaffolds due to their potential applications. The Groebke–Blackburn–Bienaymé reaction (GBBR) is a greener alternative to synthesizing IMPs.
Manuel A. Rentería-Gómez, David Calderón-Rangel, Fidel Rodríguez-López, Alejandro Corona-Díaz, Rocío Gámez-Montaño   +4 more
doaj   +1 more source