Themed collection New Talent

Artificial supramolecular protein assemblies can serve as novel high-order scaffolds that can display various functional proteins with defined valencies and organization, offering unprecedented functional bio-architectures.

We here review strategies for site-directed spin labeling (SDSL) of proteins and discuss their potential for EPR distance measurements to study protein function in vitro and in cells.

A comprehensive review covering the field of enantioselective polyene cyclizations.

The directing group assisted site selective C–H functionalization approach is having a continuous impact in the field of natural product synthesis, drug discovery and material sciences.

Diverse bioorthogonal reactions and chemical tagging approaches for protein labeling are discussed and compared in this review.

This review summarizes recent developments in synthetic methods for benzoheterole compounds of significant potential for applications in materials science.

A review of the isolation, biological activity, biosynthesis and chemical synthesis of nitropyrrole-containing natural products reported to date, including the pyrrolomycins, heronapyrroles and nitropyrrolins.

Trihaloethenes are versatile C₂-building blocks that can be simply modified via addition, elimination and transition metal-catalyzed reactions.

A new generation of chiral phase-transfer catalysts is summarized.

This review highlights the use of the oxidative boron Heck reaction in enantioselective Heck-type couplings.

A simple synthesis of primary bromides from alkenes using HBr in AcOH and atmospheric oxygen as a radical initiator.

We have investigated the dynamic nature of 1,2-oxazines, which revealed broad tunability and potential for applications in covalent adaptable materials.

The K₃PO₄-mediated intramolecular Rauhut-Currier type reaction of chalcones having an enoate moiety leading to the formation of 4H-chromenes in moderate to good yields is demonstrated.

A small synthetic calcium sensor that can be site-specifically coupled to any protein of interest in living cells by utilizing the bio-orthogonal HaloTag labeling strategy.

Total synthesis of three important trehalose containing tetrasaccharides isolated from Mycobacterium smegmatis is reported for the first time, using regioselective opening of benzylidene acetals and stereoselective glycosylations as key steps.

Intramolecular C–H trifluoromethoxylation of arenes and heteroarenes proceeds through a reaction mechanism of radical O-trifluoromethoxylation and ionic OCF₃-migration.

Chiral phenolic p-tolylsulfoxides, t-butylsulfoxides and well-defined aluminum complexes were prepared by short synthetic routes from readily available starting materials.

Thia-Pictet–Spengler cyclization is used for stereoselective synthesis of N-fused thiazinoindole derivatives. One-pot, sequential Friedel–Crafts alkylation – Pictet–Spengler cyclization and the synthesis of thiazino-oxepino-indole is developed.

We report herein a protocol for preparing alkynes from alkenyl triflates at ambient temperature with LiCl as a promoter.

The synthesis and self-assembly of a new C₂-symmetric oligohistidine amphiphile equipped with an aggregation induced emission luminophore is reported.

A new rhodium-catalyzed [4 + 2]-pyridannulation of 3-substituted indoles with diazoenals resulted in the biologically important pyrido[1,2-a]indoles.

Described herein a divergent strategy for the synthesis of furo[3,4-b]indoles via a sequential Ag(I)/Bi(III)/Pd(II) catalysis and cyclopenta[b]indoles via a one-pot Ag(I)/Brønsted acid relay catalysis, starting from the easily accessible 3-(2 aminophenyl)-4-pentenyn-3-ols.

Diphosphoinositol polyphosphates (inositol pyrophosphates, X-InsP₇) are a family of second messengers with important roles in eukaryotic biology. A new approach targeting 2-InsP₇ and a photocaged analogue is described.

As more methodologies for generating and manipulating biomimetic cellular systems are developed, opportunities arise for combining different methods to create more complex synthetic biological constructs.

The efficient conversion of siphonodictyal B into the spirocyclic natural products corallidictyals A–D has been achieved via oxidative and acid catalyzed cyclizations.

A direct method for the synthesis of diaryl- and triarylmethyl phosphonates through 1,6-hydrophosphonylation of p-quinone methides and fuchsones using NHC as a Brønsted base catalyst is described.

We use kinetic data, photophysical properties, and mechanistic analyses to compare recently developed high-rate constant oxime and hydrazone formations.

A Brønsted acid-catalyzed addition of 2-alkylazaarenes to in situ generated N-sulfonylimines through selective C(sp³)–H bond functionalization has been developed.

In this report, we describe an efficient way to generate libraries of macrocyclic glycopeptides in one step by reacting phage-displayed libraries of peptides with dichloro-oxime derivatives.

A one-pot synthesis of anilines and nitrosobenzenes from phenols has been developed using an ipso-oxidative aromatic substitution (ⁱS_OAr) process.

To reconcile the urgent need to access well defined β-configured 2,6-di-deoxypyranose analogues for chemical biology, with the intrinsic α-selectivity of the native system, the directing role of fluorine at C2 has been explored.

An efficient protocol for palladium-catalyzed PE auxiliary-directed C(sp³)–H arylation reaction with sterically hindered aryl iodides was developed.

An iron-catalyzed arylation of α-aryl-α-diazoesters with electron-rich benzene rings was developed, which provides an efficient method for the preparation of 1,1-diarylacetates with high yields and excellent chemo- and regio-selectivities.

A chiral complex derived from (S)-difluorophos and Hg(OTf)₂ is identified as a powerful catalyst for the Sakurai–Hosomi reaction of isatins with allyltrimethylsilane, allowing the facile synthesis of valuable building blocks 3-allyl-3-hydroxyoxindoles in up to 97% ee, with only 0.5–1.0 mol% of catalyst loading.

A novel Mcl-1 inhibitor chemotype based on a tetrahydroquinoline carboxylic acid was developed utilizing structure-based design, which was subsequently validated by a fluorescence polarization competition assay and HSQC NMR analysis.

A general approach to the asymmetric synthesis of highly substituted dihydroquinolines was achieved through neighboring ortho-amino group engaged sequential Michael/amination/dehydration reactions.

An iron-catalyzed transfer hydrogenation of N-aryl and N-alkyl imines using isopropanol as the hydrogen donor is reported for the first time.

Copper-catalyzed electrophilic amination using functionalized N-methoxyamines, prepared by nucleophilic addition to N-methoxyamides, is reported.

A method for the [2 + 2] cycloaddition of aryl ketenes and alkenes is presented.

anti-Aminofluorination of alkenes with amidines was enabled by hypervalent iodine(III) reagents, affording 4-fluoroalkyl-2-imidazolines. Further reductive ring-opening of the 2-imidazoline moiety could deliver highly functionalized 3-fluoropropane-1,2-diamine derivatives.

The strategy was further applied for the synthesis of optically active pyrrolo[1,2-a]indoles in >97% de using the chiral auxiliary based approach.

A multipurpose UTP analog potentially suitable for RNA aptamer selection and two-channel visualization of RNA in cells by using click chemistry and Raman spectroscopy has been developed.

The effectiveness of computational tools in determining relative configurations of complex molecules is investigated, using natural products mandelalides A–D and coibamide A, towards a generalized recipe for the scientific community at large.

C2-alkenylated heteroaromatics can be accessed by simple Brønsted acid catalysed union of diverse heteroarene N-oxides with alkenes. The scope and limitations of the process are outlined.

Photoisomerization boosts the enzymatic disassembly of smart polymeric micelles based on amphiphilic PEG–dendron hybrids bearing enzymatically cleavable azobenzene end-groups.

A strategy for the production of side-chain-to-tail cyclic peptides from ribosomally derived polypeptide precursors is reported.

The first highly regio- and enantioselective nucleophilic dearomatization of diazarenes by anion-binding organocatalysis is reported.

Computational studies highlight the importance of conformational diversity in the enantioconvergent hydrolysis of styrene oxide by potato epoxide hydrolase 1.

This paper describes the synthesis of polymers and silica nanoparticles, both bearing polystyrene sulfonate brushes, and the measurement of their binding affinity for the chemokine monocyte chemoattractant protein-1 (MCP-1) in monomeric and dimeric form.

Acetanilides and nitriles are mildly and selectively reduced over various other carbonyl derivatives using an electron-deficient boron catalyst and triethylsilane.

Side-chain cyclization has a consistent effect on protein folding energetics, and the identity of the cross-linking moiety determines the magnitude of stabilization.

The stabilization of G-quadruplex DNA structures by using small molecule ligands having simple structural scaffolds has the potential to be harnessed for developing next generation anticancer agents.

Herein we report the design, synthesis, biophysical and biological evaluation of triazole containing prolinamide derivatives as selective c-MYC G-quadruplex binding ligands.

Molecular imaging visualized significantly reduced clearance of AGE-albumin.

An asymmetric addition of naphthols to in situ generated para-quinone methides catalyzed by a chiral phosphoric acid is described.

A dimethyldihydropyrene based photochromic π-switch in its closed state forms donor–acceptor stacks with 1,4,5,8-naphthalenetetracarboxylic dianhydride. The stacks collapse in the photoisomeric open form.

An overview of synthetic efforts toward the initially proposed structure of yuremamine using iterative C(sp³)–H arylations is described.

A unified strategy for the palladium-catalyzed Suzuki–Miyaura cross-coupling of amides with boronic acids for the synthesis of ketones by N–C bond activation is reported.

Acid–base modulated host–guest binding at the micellar–water interface triggers reversible oblate ellipsoid-to-lamellar morphological transitions revealing the relationship between and morphology.

An efficient and green method for the α-hydroxylation of substituted ketones has been developed.

A highly-strained, nitrogen-doped cycloparaphenylene (CPP), aza[6]CPP, was synthesized and then converted to a donor–acceptor nanohoop, N-methylaza[6]CPP, via alkylation of the nitrogen center.

A simple and efficient iodine-assisted protocol for synthesis of 5-substituted-3-methyl/benzyl-1,3,4-oxadiazol-2(3H)-ones has been developed.

The title reaction leads to 1,6-difunctionalized products without the requirement of premetallated reagents. Details on scope, selectivity and mechanism are reported.

Lewis acid-mediated three component coupling of salicyladehydes, anilines and gylcals provided novel benzopyran-fused pyranoquinolines stereoselectively, in moderate to high yields.

A protocol for the synthesis of chiral β-aminophosphines by ring-opening of cyclic sulfamidates with metallated secondary phosphine oxides is described. It allows access to previously unknown derivatives having electron-deficient, electron-rich and sterically hindered P-aryl substituents.

A formal γ-allylation of deconjugated butenolides is reported based on a two-step sequence consisting of a catalytic diastereo- and enantioselective vinylogous nucleophilic addition to vinyl sulfones and Julia–Kocienski olefination. This highly modular approach delivers densely functionalized butenolides containing a quaternary stereogenic centre in excellent yield with high enantioselectivity.