A5021719017- Quinazolinone synthesis and applications
- Drug Transport and Resistance Mechanisms
- Biochemical and Molecular Research
- Synthesis and Characterization of Heterocyclic Compounds
- Cancer therapeutics and mechanisms
- Neurological disorders and treatments
- Hormonal and reproductive studies
- Parkinson's Disease Mechanisms and Treatments
- Chemical Reaction Mechanisms
- Botulinum Toxin and Related Neurological Disorders
- Trace Elements in Health
- Synthesis and Reactivity of Heterocycles
- Protein Kinase Regulation and GTPase Signaling
- Computational Drug Discovery Methods
- Synthesis and biological activity
- Synthesis and Biological Evaluation
- Neurotransmitter Receptor Influence on Behavior
- DNA and Nucleic Acid Chemistry
- HIV/AIDS drug development and treatment
- Crystallization and Solubility Studies
- Bioactive Compounds and Antitumor Agents
- Metal complexes synthesis and properties
- Hypothalamic control of reproductive hormones
- Plant-Derived Bioactive Compounds
- Parasitic Infections and Diagnostics
Centre National de la Recherche Scientifique
2012-2024
Université Claude Bernard Lyon 1
2009-2024
Centre de Recherche en Neurosciences de Lyon
2018-2024
Inserm
2009-2024
Hospices Civils de Lyon
2012-2024
Centre Hospitalier Le Vinatier
2024
Centre d'Exploration et de Recherche Médicale par Emission de Positons
2019-2024
Institut de Chimie de Clermont-Ferrand
2016-2023
Université Clermont Auvergne
2016-2022
Institut des Sciences Biologiques
2021
A series of indeno[1,2-b]indole-9,10-dione derivatives were synthesized as human casein kinase II (CK2) inhibitors. The most potent inhibitors contained a N5-isopropyl substituent on the C-ring. same compounds was found to also inhibit breast cancer resistance protein ABCG2 but with totally different structure–activity relationships: N5-phenethyl critical, and additional hydrophobic substituents at position 7 or 8 D-ring methoxy phenethyl ortho meta contributed inhibition. best inhibitors,...
Accumulation of α-synuclein (α-syn) is a neuropathological hallmark synucleinopathies. To date, no selective α-syn positron emission tomography (PET) radiotracer has been identified. Our objective was to develop the first original, selective, and specific PET radiotracer. Chemical design inspired from three structural families that demonstrated interesting binding characteristics used as starting point. Bioinformatics modeling fibrils then employed select best molecular candidates before...
The accumulation of aggregated alpha-synuclein ( α -syn) in multiple brain regions is a neuropathological hallmark synucleinopathies. Multiple system atrophy (MSA) synucleinopathy characterized by the predominant cerebral -syn as cytoplasmic glial inclusions (CGI). A premortem diagnosis tool would improve early and help monitoring disease progression therapeutic efficacy. One Positron Emission Tomography (PET) study suggested [ 11 C]BF-227 promising radiotracer for intracellular deposition...
Casein kinase II (CK2) is an intensively studied enzyme, involved in different diseases, cancer particular. Different scaffolds were used to develop inhibitors of this enzyme. Here, we report on the synthesis and biological evaluation twenty phenolic, ketonic, para-quinonic indeno[1,2-b]indole derivatives as CK2 inhibitors. The most active compounds 5-isopropyl-1-methyl-5,6,7,8-tetrahydroindeno[1,2-b]indole-9,10-dione 4h...
Highly substituted purines were synthesized in good to high yields through a one-pot straightforward metal-free scalable method, using the Traube synthesis adapted Vilsmeier-type reagents. From 5-amino-4-chloropyrimidines, new 9-aryl-substituted chloropurines and intermediates for peptide nucleic acid prepared. Variant procedures allowing rapid of ribonucleosides 7-benzylpurine from 5-amidino-6-aminopyrimidines are also reported illustrate potential this versatile toolbox. This route appears...
Aim: Bronchial epithelium acts as a defensive barrier against inhaled pollutants and microorganisms. This is often compromised in inflammatory airway diseases that are characterized by excessive oxidative stress responses, leading to bronchial epithelial shedding, failure, increased permeability. Among proteins expressed the junctional participating regulation of response environmental stresses cellular prion protein (PrPC). However, role PrPC still unknown epithelium. Herein, we...
The Fourier transformation (FT) is a mathematical process frequently encountered by chemistry students. However, it remains an automated background perceived many students as difficult to understand. In this paper we present simple open-source web application, which can help understand the basics of FT applied nuclear magnetic resonance (NMR) spectroscopy.
The understanding of the basic principles chromatography is high importance for chemistry, pharmacy, and biology students. In this paper, we present a free web application which can be used as teaching tool to introduce undergraduate students, using one simplest models: plate theory.
Abstract Background Estimates suggest that approximatively 25% of the world population will be overweight in 2025. Better understanding pathophysiology obesity help to develop future therapeutics. Serotonin subtype 6 receptors (5-HT ) have been shown critically involved appetite reduction and weight loss. However, it is not known if pathological cascade triggered by modifies density 5-HT brain. Methods Influence diet-induced (DIO) Wistar rats was explored using MRI (whole-body fat) PET ([ 18...
A one-pot glycosylation and cyclization procedure is described for the synthesis of 6-chloropurine ribonucleosides from chloropyrimidines. From such a modification obtained chloropurine ribonucleosides, many drug candidates or molecular tools biological study designed their similarity to naturally occurring nucleosides could be obtained. The begins by preparation several amidinoaminochloropyrimidines as precursors procedure. Then, adding trimethylsilyl trifluoromethanesulfonate (TMSOTf)...
Searchable abstracts of presentations at key conferences in endocrinology ISSN 1470-3947 (print) | 1479-6848 (online)