Cycloadditions of cyclohexynes and cyclopentyne. [PDF]
We report the strategic use of cyclohexyne and the more elusive intermediate, cyclopentyne, as a tool for the synthesis of new heterocyclic compounds. Experimental and computational studies of a 3-substituted cyclohexyne are also described.
Garg, Neil K +4 more
core +2 more sources
Atroposelective interrupted CuAAC reaction using cyclic diaryliodoniums
Copper-catalyzed azide–alkyne cycloaddition (CuAAC) is a pivotal strategy for joining two fragments, including bioactive moieties under mild conditions.
Yuanyuan Li +3 more
doaj +1 more source
Kinetic and Thermodynamic Approaches for the Efficient Formation of Mechanical Bonds [PDF]
Among the growing collection of molecular systems under consideration for nanoscale device applications, mechanically interlocked compounds derived from electrochemically switchable bistable [2]rotaxanes and [2]catenanes show great promise. These systems
Aprahamian, Ivan +7 more
core +1 more source
Synthesis of Polysulfone Based Amphiphilic Graft Copolymers by a ‘Grafting to’ Approach
Synthesis of amphiphilic polysulfone graft copolymers by ‘‘Click’’ chemistry is described. First, a commercial PSU was chloromethylated to give chloro-funtional PSU (PSU-Cl).
Mustafa Ciftci
doaj +1 more source
A ribose-functionalized NAD+ with unexpected high activity and selectivity for protein poly-ADP-ribosylation. [PDF]
Nicotinamide adenine dinucleotide (NAD+)-dependent ADP-ribosylation plays important roles in physiology and pathophysiology. It has been challenging to study this key type of enzymatic post-translational modification in particular for protein poly-ADP ...
Chen, Jingwen +9 more
core +1 more source
Relative Rates of Metal-Free Azide-Alkyne Cycloadditions: Tunability over 3 Orders of Magnitude. [PDF]
The thermal (3 + 2) dipolar azide-alkyne cycloaddition, proceeding without copper or strained alkynes, is an underutilized ligation with potential applications in materials, bioorganic, and synthetic chemistry.
Braslau, Rebecca +6 more
core
A Synergistic Inhibitor Development Strategy Against Human UDP‐Galactose‐4‐Epimerase
The epimerase GalE is crucial for the biosynthesis of cancer‐relevant O‐GalNAc glycans. Here, we employ orthogonal, structurally enabled small molecule fragment screens to yield both covalent and non‐covalent inhibitors against GalE within no more than 22 elaborated compounds.
William M. Browne +22 more
wiley +1 more source
A flow platform for degradation-free CuAAC bioconjugation
Cu-catalyzed azide-alkyne cycloaddition (CuAAC) reaction is a common bioconjugation technique; however oxidative degradation and residual copper may limit its use.
Marine Z. C. Hatit +5 more
doaj +1 more source
Regioselective Formation of 2,5-Disubstituted Oxazoles Via Copper(I)-Catalyzed Cycloaddition of Acyl Azides and 1-Alkynes [PDF]
The reaction of 1-alkynes with acylazides in the presence of [Tpm*,BrCu(NCMe)]BF4 (Tpm*,Br = tris(3,5-dimethyl-4-bromopyrazolyl)methane) as the catalyst provides 2,5-oxazoles in moderate to high yields.
Cano Rico, Israel +3 more
core +1 more source
G protein‐coupled receptors (GPCRs) are major therapeutic targets. Modulating GPCR activity through intracellular sites is evolving. A structure‐ and computation‐assisted approach generated small G protein‐derived peptidomimetics targeting the intracellular binding crevice of the β2 adrenergic receptor mimicking features of the full G protein.
Phuong Thu Tran +11 more
wiley +1 more source

