A5002256090- Synthetic Organic Chemistry Methods
- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Catalytic Cross-Coupling Reactions
- Catalytic Alkyne Reactions
- Catalytic C–H Functionalization Methods
- Oxidative Organic Chemistry Reactions
- Cannabis and Cannabinoid Research
- Microbial Natural Products and Biosynthesis
- Asymmetric Synthesis and Catalysis
- Synthesis and Biological Evaluation
- Chemical synthesis and alkaloids
- Multicomponent Synthesis of Heterocycles
- Synthesis and Biological Activity
- Marine Sponges and Natural Products
- Pharmacological Receptor Mechanisms and Effects
- Neuroscience and Neuropharmacology Research
- Metal complexes synthesis and properties
- Eicosanoids and Hypertension Pharmacology
- Microwave-Assisted Synthesis and Applications
- Metabolomics and Mass Spectrometry Studies
- Synthesis and Catalytic Reactions
- Analytical Chemistry and Chromatography
- Cancer, Lipids, and Metabolism
- Chemical Synthesis and Analysis
University of Aberdeen
2013-2024
National Yang Ming Chiao Tung University
2011-2021
Guangxi Normal University
2016
Zhejiang University
2013-2014
Seoul National University
2011-2012
Chemical Synthesis Lab
2010-2011
Institute of Chemical and Engineering Sciences
2010-2011
Agency for Science, Technology and Research
2010-2011
Imperial Valley College
2011
Imperial College London
2007-2009
The first generation of CB1 positive allosteric modulators (e.g., ZCZ011) featured a 3-nitroalkyl-2-phenyl-indole structure. Although small number drugs include the nitro group, it is generally not regarded as being "drug-like", and this particularly true for aliphatic groups. There are very few case studies where an appropriate bioisostere replaced group that had direct role in binding. This may be indicative difficulty replicating its binding interactions. Herein, we report design...
A novel one-pot, three-component reaction employing variously substituted benzimidazole-linked amino pyridines, aldehydes, and isonitriles catalyzed by scandium(III) triflate under solvent-free conditions were accomplished. This new synthetic methodology facilitates the rapid generation of intricate molecular frameworks in three-dimensional fashion leading to benzimidazole-imidazo[1,2-a] pyridines. approach is envisioned as an environmentally benign process a simple operation biological...
The concise and divergent total synthesis of (−)-indoxamycins A, C, F has been completed for the first time by using a tricyclic enone as common late-stage intermediate. key steps strategy are based on an Ireland–Claisen rearrangement, stereodivergent reductive 1,6-enyne cyclization, tandem 1,2-addition/oxa-Michael/methylenation reaction. As service to our authors readers, this journal provides supporting information supplied authors. Such materials peer reviewed may be re-organized online...
A new class of arylgermane derivative that participate efficiently in Pd(0)-catalysed cross-coupling reactions with aryl bromides following photochemical activation is described.
A novel and efficient diversity-oriented synthetic approach was employed to access the benzo[d]oxazol-5-yl-1H-benzo[d]imidazole on ionic liquid support, which helps absorb microwave irradiation. In this paper, we successfully coupled 4-hydroxy-3-nitrobenzoic acid onto liquid-immobilized o-phenylenediamine, subsequently underwent an mediated, ring closure reaction leading benzimidazole derivatives. After hydrogenation of nitro group amine, resulting conjugate reacted with...
While most research and treatments for multiple sclerosis (MS) focus on autoimmune reactions causing demyelination, it is possible that neurodegeneration precedes the response. Hence, glutamate receptor antagonists preventing excitotoxicity showed promise in MS animal models, though blocking signaling prevents critical neuronal functions. This study reports discovery of a small molecule AMPA-mediated by targeting an allosteric binding site. A machine learning approach was used to screen...
A modular strategy leading to the salvileucalin B core structure has been accomplished. The developed synthetic featured a bioinspired intramolecular Diels–Alder reaction construct domain "A", REDOX chemistry functionalize "B", and palladium-mediated cross-coupling install "C". This flexible approach should facilitate further chemical biological investigations of this fascinating class compounds.
The enormous prevalence of infections caused by parasitic nematodes worldwide, coupled to the rapid emergence their resistance commonly used anthelmintic drugs, presents an urgent need for discovery new drugs. Herein, we have identified several classes small molecules with broad spectrum activity against these pathogens. Previously, reported identification carnitine palmitoyltransferases (CPTs) as a representative class enzymes potential targets metabolic chokepoint intervention that was...
Abstract The Pd(0) catalysed cross‐coupling of arylgermanes with aryl bromides is shown to require at least two labile heteroatom ligands on the Ge centre allow efficient nucleophilic activation by fluoride. Dichloroarylgermanes 7a and 7b are cross‐couple a series moderate efficiency using KF in DMF. Bis(2‐naphthylmethyl)arylgermane 18b identified as ‘safety‐catch’ precursor this type substrate. 2‐naphthylmethyl substituents can be removed via photolytic oxidation presence Cu(BF 4 ) 2...
Abstract Nitrogen and sulfur co‐doped graphene supported Pd oxide‐rich (PdO x ‐rich) nanoparticles (Pd/NS‐rGO) are synthesized by microwave‐assisted ascorbic acid reduction method. Raman spectrum reveals that the introduced NS co‐doping could introduce more defects on surface. X‐ray diffraction, photoelectron spectrum, SEM TEM images indicate PdO ‐rich particles well‐dispersed Cyclic voltammograms curves illustrate Pd/NS‐rGO catalyst exhibits a larger electrochemically active surface area...
Abstract Akt is an intracellular signalling pathway that serves as essential link between cell surface receptors and cellular processes including proliferation, development survival. The has many downstream targets glycogen synthase kinase3 which a major regulatory kinase for cycle transit well controlling activity. frequently up-regulated in cancer due to overexpression of such the epidermal growth factor receptor, or mutation kinases resulting inappropriate survival proliferation....
Eine effiziente und divergente Totalsynthese der (−)-Indoxamycine A, C F wurde durch die Verwendung eines tricyclischen Enons als gemeinsames spätes Intermediat ermöglicht. Die Schlüsselschritte Synthese sind eine Ireland-Claisen-Umlagerung, stereodivergente reduktive 1,6-Enin-Cyclisierung Tandemreaktion bestehend aus 1,2-Addition, Oxa-Michael-Reaktion Methylenierung. As a service to our authors and readers, this journal provides supporting information supplied by the authors. Such materials...
A method for the parallel solid-phase synthesis (SPS) of iodinated analogues Sanofi-Aventis' type 1 cannabinoid (CB1) receptor inverse agonist rimonabant (acomplia) has been developed. The allows a range C3 amide/hydrazide derivatives from resin-bound ester precursor. C−Ge linkage to Hypogel-200 resin is stable diversification conditions but ipso-iododegermylative cleavage using NaI/NCS even products containing oxidatively labile hydrazide moiety.
Glycogen synthase kinase 3 (GSK3) is a key controlling element of many cellular processes including cell-cycle progression and recent studies suggest that GSK3 potential anticancer target. Changes in glucose metabolism associated with inhibition may impact on lipid synthesis, whilst metabolites can act as molecular response markers. Here, SKBr3 breast HCT8 colorectal cancer cells were treated the inhibitor SB216763, [14C (U)] [3H] choline incorporation into lipids was determined. Cell...
Abstract The stereocontrolled synthesis of (E)-configured styrenes via Pd(0)-catalyzed cross-couping (E)-alkenylgermanes with aryl bromides is described. germanes employed have bis(naphthalen-2-ylmethyl) substitution to allow photooxidative activation toward coupling and a C8F17-fluorous tag facilitate purification by fluorous solid-phase extraction (F-SPE). selectivities obtained suggest that germyl-Stille rather than Heck-type mechanism predominates in the step.
We designed and synthesized perhexiline analogues that have the same therapeutic profile as parent cardiovascular drug but lacking its metabolic liability associated with CYP2D6 metabolism. Cycloalkyl 6a-j were found to be unsuitable for further development, they retained a pharmacokinetic very similar shown by compound. Multistep synthesis of incorporating fluorine atoms onto cyclohexyl ring(s) provided range different fluoroperhexiline analogues. Of these, 50 (4,4-gem-difluoro) 62...
Reizvolle Strukturen: Die formalen Synthesen von 1 und 2 gelangen mithilfe einer Kaskadenstrategie, die 3 ausgeht eine Enincycloisomerisierung sowie intramolekulare Diels-Alder-Reaktion umfasst. Das Produkt 4 ging im weiteren Syntheseverlauf Ringverengung ein, ein bereits bekanntes Intermediat lieferte. Resultat ist formale Synthese der strukturell faszinierenden Titelverbindungen. Detailed facts of importance to specialist readers are published as ”Supporting Information”. Such documents...
Racemic perhexiline has been used (or is currently undergoing clinical trials) for the treatment of a variety cardiovascular disorders. Increasing evidence suggests that (–)-enantiomer should be used, as opposed to racemic mixture. Here, we report first asymmetric synthesis both enantiomers in high enantiomeric excess and assignment their (–)-<i>S</i>/(+)-<i>R</i> absolute stereochemistry by X-ray crystallography.
Androgen receptor (AR) activation is the primary driving factor in prostate cancer which initially responsive to castration but then becomes resistant (castration-resistant (CRPC)). CRPC cells still retain functioning AR can be targeted by other therapies. A recent promising development use of inhibitors (Epi-1) protein-protein interaction inhibit AR-activated signalling. Translating novel therapies into clinic requires sensitive early response indicators. Here potential markers are...