Transient receptor potential canonical type 3 channels control the vascular contractility of mouse mesenteric arteries [PDF]
Transient receptor potential canonical type 3 (TRPC3) channels are non-selective cation channels and regulate intracellular Ca2+ concentration. We examined the role of TRPC3 channels in agonist-, membrane depolarization (high K+)-, and mechanical ...
Abramowitz, Joel+6 more
core +5 more sources
Microwave-assisted synthesis of a MK2 inhibitor by Suzuki-Miyaura coupling for study in Werner syndrome cells [PDF]
Microwave-assisted Suzuki-Miyaura cross-coupling reactions have been employed towards the synthesis of three different MAPKAPK2 (MK2) inhibitors to study accelerated aging in Werner syndrome (WS) cells, including the cross-coupling of a 2-chloroquinoline
Bagley, Mark C+5 more
core +7 more sources
Effect of building block transformation in covalent triazine‐based frameworks for enhanced CO2 uptake and metal‐free heterogeneous catalysis [PDF]
Invited for the cover of this issue is the group of Pascal Van Der Voort at the University of Ghent and colleagues at Technische Universitat Berlin. The image depicts the covalent triazine frameworks reported in the manuscript for the sorption of CO2 and
Jena, Himanshu+5 more
core +2 more sources
As pyrazole and its derivatives have a wide range of biological activities, including anticancer activity, the design of novel pyrazole derivatives has emerged as an important research field.
Minsung Kang+13 more
doaj +1 more source
An operationally simple and metal-free approach is described for the synthesis of pyrazole-tethered thioamide and amide conjugates. The thioamides were generated by employing a three-component reaction of diverse pyrazole C-3/4/5 carbaldehydes, secondary
Shubham Sharma+8 more
doaj +1 more source
Recent Applications of the Multicomponent Synthesis for Bioactive Pyrazole Derivatives
Pyrazole and its derivatives are considered a privileged N-heterocycle with immense therapeutic potential. Over the last few decades, the pot, atom, and step economy (PASE) synthesis of pyrazole derivatives by multicomponent reactions (MCRs) has gained ...
Diana Becerra+2 more
doaj +1 more source
Lead identification and structure-activity relationships of heteroarylpyrazole arylsulfonamides as allosteric CC-chemokine receptor 4 (CCR4) antagonists [PDF]
A knowledge-based library of aryl 2,3-dichlorophenylsulfonamides was synthesised and screened as human CCR4 antagonists, in order to identify a suitable hit for the start of a lead-optimisation programme.
Copley, R.C.B.+4 more
core +1 more source
Rational Design, Synthesis and Biological Evaluation of Pyrimidine-4,6-diamine derivatives as Type-II inhibitors of FLT3 Selective Against c-KIT. [PDF]
FMS-like Tyrosine Kinase 3 (FLT3) is a clinically validated target for acute myeloid leukemia (AML). Inhibitors targeting FLT3 have been evaluated in clinical studies and have exhibited potential to treat FLT3-driven AML.
Bharate, Jaideep B+8 more
core +2 more sources
The structure of the agrochemical fungicidal 4-Chloro-3-(3,5-dichloropheny)-1H-pyrazole, RPA 406194 and related compounds [PDF]
The difficulties to obtain convenient monocrystals of the important fungicide RPA 406194 have been overcome by a combination of solid state 13C NMR, X-ray powder diffraction and molecular modeling.
Abboud+35 more
core +2 more sources