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