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Themed collection New Talent: Europe

24 items
Profile

Contributors to ‘New Talent: Europe’

MedChemComm profiles the contributors to the ‘New Talent: Europe’ themed issue.

Graphical abstract: Contributors to ‘New Talent: Europe’
From the themed collection: New Talent: Europe
Review Article

Bioorthogonal metabolic labelling with acyl-CoA reporters: targeting protein acylation

Bioorthogonal labels in protein acylation: advantages and disadvantages of metaBO(W)lic tagging with acyl-CoA(RROWS).

Graphical abstract: Bioorthogonal metabolic labelling with acyl-CoA reporters: targeting protein acylation
From the themed collection: New Talent: Europe
Open Access Research Article

Methods of protein surface PEGylation under structure preservation for the emulsion-based formation of stable nanoparticles

We evaluated different methods for a high surface PEGylation of lysozyme. The resulting lipophilic enzymes can be used for the formation of stable nanoparticles.

Graphical abstract: Methods of protein surface PEGylation under structure preservation for the emulsion-based formation of stable nanoparticles
From the themed collection: New Talent: Europe
Open Access Research Article

Design and synthesis of fused soluble epoxide hydrolase/peroxisome proliferator-activated receptor modulators

Metabolic syndrome (MetS) is a widespread, complex disease cluster which consists of hypertension, atherosclerosis, dyslipidaemia and type II diabetes.

Graphical abstract: Design and synthesis of fused soluble epoxide hydrolase/peroxisome proliferator-activated receptor modulators
From the themed collection: New Talent: Europe
Open Access Research Article

Squaramides with cytotoxic activity against human gastric carcinoma cells HGC-27: synthesis and mechanism of action

A series of squaramates and squaramides have been synthesized and their cytotoxic activity has been investigated in different cancer cell lines.

Graphical abstract: Squaramides with cytotoxic activity against human gastric carcinoma cells HGC-27: synthesis and mechanism of action
From the themed collection: New Talent: Europe
Research Article

Injectable peptide hydrogels for controlled-release of opioids

Peptide-based hydrogels as a drug carrier system for the subcutaneous administration of morphine.

Graphical abstract: Injectable peptide hydrogels for controlled-release of opioids
From the themed collection: New Talent: Europe
Research Article

Aryl and heteroaryl N-[4-[4-(2,3-substituted-phenyl)piperazine-1-yl]alkyl]carbamates with improved physico-chemical properties as dual modulators of dopamine D3 receptor and fatty acid amide hydrolase

Improving the physico-chemical profile of a MTDL series.

Graphical abstract: Aryl and heteroaryl N-[4-[4-(2,3-substituted-phenyl)piperazine-1-yl]alkyl]carbamates with improved physico-chemical properties as dual modulators of dopamine D3 receptor and fatty acid amide hydrolase
From the themed collection: New Talent: Europe
Open Access Research Article

Design and synthesis of triazole-based peptidomimetics of a PSD-95 PDZ domain inhibitor

A novel PSD-95 PDZ2 peptidomimetic has been discovered by designing azide and alkyne amino acid analogues and click chemistry.

Graphical abstract: Design and synthesis of triazole-based peptidomimetics of a PSD-95 PDZ domain inhibitor
From the themed collection: New Talent: Europe
Research Article

Development of a competitive binding assay for the Burkholderia cenocepacia lectin BC2L-A and structure activity relationship of natural and synthetic inhibitors

Burkholderia cenocepacia is an opportunistic Gram-negative pathogen and especially hazardous for cystic fibrosis patients.

Graphical abstract: Development of a competitive binding assay for the Burkholderia cenocepacia lectin BC2L-A and structure activity relationship of natural and synthetic inhibitors
From the themed collection: New Talent: Europe
Open Access Research Article

Targeting the protein backbone with aryl halides: systematic comparison of halogen bonding and π⋯π interactions using N-methylacetamide

Systematic plane scans reveal a seamless transition from σ-hole interactions with the carbonyl oxygen to interactions with the amide π-electrons at increasing distances.

Graphical abstract: Targeting the protein backbone with aryl halides: systematic comparison of halogen bonding and π⋯π interactions using N-methylacetamide
From the themed collection: New Talent: Europe
Research Article

Fragment pharmacophore-based in silico screening: a powerful approach for efficient lead discovery

A fragmentation–recombination process coupled with fragment-based pharmacophore in silico screening: a tailor-made approach for the discovery of new cosmetics.

Graphical abstract: Fragment pharmacophore-based in silico screening: a powerful approach for efficient lead discovery
From the themed collection: New Talent: Europe
Open Access Research Article

Drug trapping in hERG K+ channels: (not) a matter of drug size?

The hERG cavity can trap very bulky compounds, without perturbing normal gate closure.

Graphical abstract: Drug trapping in hERG K+ channels: (not) a matter of drug size?
From the themed collection: New Talent: Europe
Open Access Research Article

eCF309: a potent, selective and cell-permeable mTOR inhibitor

Kinase inhibitors capable of blocking the phosphorylation of protein substrates with high selectivity are essential to probe and elucidate the etiological role of such molecules and their signalling pathways.

Graphical abstract: eCF309: a potent, selective and cell-permeable mTOR inhibitor
From the themed collection: New Talent: Europe
Research Article

Rigid amphipathic nucleosides suppress reproduction of the tick-borne encephalitis virus

Rigid amphipathic fusion inhibitors (RAFIs), 5-arylethynyl uracil nucleosides with bulky aryl groups, appeared to have considerable activity against tick-borne encephalitis virus (TBEV) in cell culture.

Graphical abstract: Rigid amphipathic nucleosides suppress reproduction of the tick-borne encephalitis virus
From the themed collection: New Talent: Europe
Research Article

A multicomponent pharmacophore fragment-decoration approach to identify selective LRRK2-targeting probes

Herein we report the development of a new versatile chemical tool for the rapid identification of LRRK2-targeting probes as potential anti-Parkinson's agents.

Graphical abstract: A multicomponent pharmacophore fragment-decoration approach to identify selective LRRK2-targeting probes
From the themed collection: New Talent: Europe
Open Access Research Article

A potent trifluoromethyl ketone histone deacetylase inhibitor exhibits class-dependent mechanism of action

Kinetic evaluation of HDAC inhibitors containing different zinc-binding chemotypes demonstrates that trifluoromethyl ketone-containing compounds can inhibit individual HDAC isozymes via differential mechanisms.

Graphical abstract: A potent trifluoromethyl ketone histone deacetylase inhibitor exhibits class-dependent mechanism of action
From the themed collection: New Talent: Europe
Research Article

Tetrahydro-pyrimido-indoles as selective LIMK inhibitors: synthesis, selectivity profiling and structure–activity studies

Extensive structure–activity studies on three different modification sites resulted in a series of LIM kinase inhibitors, containing a novel tricyclic hinge-binding motif based on the pyrrolopyrimidine scaffold.

Graphical abstract: Tetrahydro-pyrimido-indoles as selective LIMK inhibitors: synthesis, selectivity profiling and structure–activity studies
From the themed collection: New Talent: Europe
Open Access Research Article

Antiprotozoal activity of dehydroabietic acid derivatives against Leishmania donovani and Trypanosoma cruzi

Dehydroabietic acid derivatives have potent antiprotozoal activity and selectivity against L. donovani and T. cruzi.

Graphical abstract: Antiprotozoal activity of dehydroabietic acid derivatives against Leishmania donovani and Trypanosoma cruzi
From the themed collection: New Talent: Europe
Research Article

Probing for improved selectivity with dipeptide-derived inhibitors of dipeptidyl peptidases 8 and 9: the impact of P1-variation

The influence of P1-variation on DPP8/9 inhibitor selectivity is investigated.

Graphical abstract: Probing for improved selectivity with dipeptide-derived inhibitors of dipeptidyl peptidases 8 and 9: the impact of P1-variation
From the themed collection: New Talent: Europe
Open Access Research Article

Demonstration of the dynamic mass redistribution label-free technology as a useful cell-based pharmacological assay for endogenously expressed GABAA receptors

Within the continuous quest for the discovery of pharmacologically interesting compounds, the development of new and superior drug screening assays is desired.

Graphical abstract: Demonstration of the dynamic mass redistribution label-free technology as a useful cell-based pharmacological assay for endogenously expressed GABAA receptors
From the themed collection: New Talent: Europe
Research Article

Novel indole–flutimide heterocycles with activity against influenza PA endonuclease and hepatitis C virus

Structure-based design and synthesis of novel indole–flutimide derivatives with antiviral activity.

Graphical abstract: Novel indole–flutimide heterocycles with activity against influenza PA endonuclease and hepatitis C virus
From the themed collection: New Talent: Europe
Research Article

Integrating multicomponent flow synthesis and computational approaches for the generation of a tetrahydroquinoline compound based library

The combination of flow chemistry and computational tools has been successfully applied to prepare a focused library of tricyclic tetrahydroquinolines endowed with drug-like properties.

Graphical abstract: Integrating multicomponent flow synthesis and computational approaches for the generation of a tetrahydroquinoline compound based library
From the themed collection: New Talent: Europe
Research Article

Spirooxadiazoline oxindoles with promising in vitro antitumor activities

This paper reports the synthesis and biological evaluation of thirty one spirooxadiazoline oxindoles as potential anticancer agents.

Graphical abstract: Spirooxadiazoline oxindoles with promising in vitro antitumor activities
From the themed collection: New Talent: Europe
Research Article

In silico-driven multicomponent synthesis of 4,5- and 1,5-disubstituted imidazoles as indoleamine 2,3-dioxygenase inhibitors

A virtual library of 50 000 000 compounds synthesizable via the van Leusen MCR was created, screened and filtered to afford a series of disubstituted imidazoles with improved properties compared to 4-phenylimidazole.

Graphical abstract: In silico-driven multicomponent synthesis of 4,5- and 1,5-disubstituted imidazoles as indoleamine 2,3-dioxygenase inhibitors
From the themed collection: New Talent: Europe
24 items

About this collection

This themed issue, guest edited by Professors Gerhard Ecker, Koen Augustyns and Uli Stilz, showcases some of the top research from emerging investigators from Europe. This issue covers medicinal chemistry research in its broadest sense, and showcases the strength of research being carried out by tomorrow's leaders in the field

Articles in this themed issue will be added below as soon as possible after they are published. Please return to this page frequently to see the collection grow.

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