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Themed collection New Talent: Americas

16 items
Cover

Front cover

Graphical abstract: Front cover
From the themed collection: New Talent: Americas
Cover

Inside front cover

Graphical abstract: Inside front cover
From the themed collection: New Talent: Americas
Profile

Contributors to ‘New Talent: Americas’

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

Graphical abstract: Contributors to ‘New Talent: Americas’
From the themed collection: New Talent: Americas
Research Article

Development of inverse electron demand Diels–Alder ligation and TR-FRET assays for the determination of ligand–protein target occupancy in live cells

We describe IED-DA ligation-based pull-down and TR-FRET assays for in-cell determination of target occupancy by the reversible inhibitor Dasatinib.

Graphical abstract: Development of inverse electron demand Diels–Alder ligation and TR-FRET assays for the determination of ligand–protein target occupancy in live cells
From the themed collection: New Talent: Americas
Research Article

The discovery of a pan-genotypic, primer grip inhibitor of HCV NS5B polymerase

A series of novel 7-azabenzofurans exhibiting pan-genotype inhibition of HCV NS5B polymerase via binding to the primer grip site is presented.

Graphical abstract: The discovery of a pan-genotypic, primer grip inhibitor of HCV NS5B polymerase
From the themed collection: New Talent: Americas
Open Access Research Article

Nonomuraea sp. ATCC 55076 harbours the largest actinomycete chromosome to date and the kistamicin biosynthetic gene cluster

We report the largest actinomycete genome to date, which encodes >30 secondary metabolites, including the kistamicin biosynthetic gene cluster.

Graphical abstract: Nonomuraea sp. ATCC 55076 harbours the largest actinomycete chromosome to date and the kistamicin biosynthetic gene cluster
From the themed collection: New Talent: Americas
Research Article

Quantitative measurement of intracellular HDAC1/2 drug occupancy using a trans-cyclooctene largazole thiol probe

We developed a transcylcooctene-based chemical probe for quantitative measurement of intracellular HDAC1/2 occupancy.

Graphical abstract: Quantitative measurement of intracellular HDAC1/2 drug occupancy using a trans-cyclooctene largazole thiol probe
From the themed collection: New Talent: Americas
Research Article

Identification of imidazo[1,2-b]pyridazine TYK2 pseudokinase ligands as potent and selective allosteric inhibitors of TYK2 signalling

Synthesis and SAR of selective ligands of the pseudokinase domain of the Janus kinase (JAK) TYK2 are first reported herein.

Graphical abstract: Identification of imidazo[1,2-b]pyridazine TYK2 pseudokinase ligands as potent and selective allosteric inhibitors of TYK2 signalling
From the themed collection: New Talent: Americas
Research Article

Discovery and hit-to-lead evaluation of piperazine amides as selective, state-dependent NaV1.7 inhibitors

Optimization of a screening hit led to the identification of NaV1.7 inhibitors with a desirable balance of properties.

Graphical abstract: Discovery and hit-to-lead evaluation of piperazine amides as selective, state-dependent NaV1.7 inhibitors
From the themed collection: New Talent: Americas
Research Article

Identification of potent tricyclic prodrug S1P1 receptor modulators

Herein, S1P1 partial agonists with shorter half-life than our previous clinical candidate are reported. The pulmonary and cardiac safety are assessed, issues currently observed with commercial Gilenya.

Graphical abstract: Identification of potent tricyclic prodrug S1P1 receptor modulators
From the themed collection: New Talent: Americas
Research Article

Design and synthesis of cenocladamide analogues and their evaluation against breast cancer cell lines

Synthesis of a concise series based on the natural product cenocladamide, their evaluation against a panel of breast cancer cells and preliminary mechanistic studies are discussed in this work.

Graphical abstract: Design and synthesis of cenocladamide analogues and their evaluation against breast cancer cell lines
From the themed collection: New Talent: Americas
Research Article

Small structural changes of the imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitors produce an improved safety profile

Preclinical pharmacokinetic, efficacy, and toxicology results are reported for a series of DGAT2 inhibitors for the potential treatment of hypertriglyceridemia.

Graphical abstract: Small structural changes of the imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitors produce an improved safety profile
From the themed collection: New Talent: Americas
Research Article

Chitosan nanoparticles for nitric oxide delivery in human skin

The use of nanoparticle-based transdermal delivery systems is a promising approach to efficiently carry and deliver therapeutic agents for dermal and systemic administration.

Graphical abstract: Chitosan nanoparticles for nitric oxide delivery in human skin
From the themed collection: SBQ-RSC: Celebrating UK-Brazil collaborations
Research Article

Discovery of cyclopropyl chromane-derived pyridopyrazine-1,6-dione γ-secretase modulators with robust central efficacy

γ-Secretase modulators for the treatment of Alzheimer's disease.

Graphical abstract: Discovery of cyclopropyl chromane-derived pyridopyrazine-1,6-dione γ-secretase modulators with robust central efficacy
From the themed collection: New Talent: Americas
Research Article

Microwave-enhanced Friedländer synthesis for the rapid assembly of halogenated quinolines with antibacterial and biofilm eradication activities against drug resistant and tolerant bacteria

We disclose a microwave-enhanced Friedländer reaction that led to new antibacterials and biofilm-eradicators.

Graphical abstract: Microwave-enhanced Friedländer synthesis for the rapid assembly of halogenated quinolines with antibacterial and biofilm eradication activities against drug resistant and tolerant bacteria
From the themed collection: New Talent: Americas
Research Article

Molecular hybridization as a powerful tool towards multitarget quinoidal systems: synthesis, trypanocidal and antitumor activities of naphthoquinone-based 5-iodo-1,4-disubstituted-, 1,4- and 1,5-disubstituted-1,2,3-triazoles

Some of the hybrid compounds exhibited promising trypanocidal and anticancer activities.

Graphical abstract: Molecular hybridization as a powerful tool towards multitarget quinoidal systems: synthesis, trypanocidal and antitumor activities of naphthoquinone-based 5-iodo-1,4-disubstituted-, 1,4- and 1,5-disubstituted-1,2,3-triazoles
From the themed collection: New Talent: Americas
16 items

About this collection

This themed issue, guest edited by Professors Sylvie Garneau-Tsodikova (University of Kentucky) and Patrick Gunning (University of Toronto), and Dr Mark Bunnage (Pfizer), showcases some of the top research from emerging investigators from the Americas. 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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