A5078241551- Synthesis and biological activity
- Click Chemistry and Applications
- Synthesis of Organic Compounds
- Coordination Chemistry and Organometallics
- Marine Sponges and Natural Products
- Asymmetric Synthesis and Catalysis
- Computational Drug Discovery Methods
- Ion channel regulation and function
- Fungal Plant Pathogen Control
- Synthetic Organic Chemistry Methods
- Chemical synthesis and alkaloids
- X-ray Diffraction in Crystallography
- Synthesis and Characterization of Heterocyclic Compounds
- Pain Mechanisms and Treatments
- Pharmacological Receptor Mechanisms and Effects
- Synthesis and Biological Evaluation
- Crystallization and Solubility Studies
- Photodynamic Therapy Research Studies
- Porphyrin and Phthalocyanine Chemistry
- Cancer Treatment and Pharmacology
- Protein Kinase Regulation and GTPase Signaling
- Natural product bioactivities and synthesis
- Protein Tyrosine Phosphatases
- Carbohydrate Chemistry and Synthesis
- Marine Toxins and Detection Methods
Institut de Chimie de Clermont-Ferrand
2013-2024
Université Clermont Auvergne
2013-2023
Centre National de la Recherche Scientifique
2013-2020
Clermont Université
2009-2020
Sigma Clermont
2016-2020
Clermont-Ferrand’s Superior National School of Chemistry
2009-2015
University of Salford
2004-2010
Arizona State University
2000-2009
Cancer Research Institute
2009
University of Manchester
1996-2009
The TWIK-related K+ channel, TREK-1, has recently emerged as an attractive therapeutic target for the development of a novel class analgesic drugs, suggesting that activation TREK-1 could result in pain inhibition. Here, we report synthesis series substituted acrylic acids (1-54) based on our previous work with caffeate esters. analogues were evaluated their ability to modulate channel by electrophysiology and vivo antinociceptive activity (acetic acid-induced writhing hot plate assays),...
A molecular modeling study was carried out to develop a predictive model for combretastatin-like analogues populating the colchicine-binding site of β-tubulin. series compounds built around framework including two aromatic groups linked by various moieties such as alkenes (stilbenes), enones (chalcones), or ethers selected study. The 5D-QSAR developed stepwise. First generated chalcone (19 compounds, 71 conformations), then stilbene (18 59 and finally combined dataset (47 ligands, 160...
Photodynamic therapy (PDT) and vascular-disrupting agents (VDA) each have their advantages in the treatment of solid tumors, but also present drawbacks. In PDT, hypoxia at center tumor limits conversion molecular oxygen into singlet oxygen, while VDAs are deficient affecting rim tumor. A phthalocyanine-chalcone conjugate combining VDA properties chalcones with PDT phthalocyanines was designed to address these deficiencies. Its vascular targeting, photophysical, photochemical, photodynamic...
To further pursue the antineoplastic leads offered by our isolation of trans-dihydronarciclasine (1a) and 7-deoxy-trans-dihydronarciclasine (1c) from two medicinal plant species Amaryllidaceae family, a practical palladium-catalyzed hydrogenation procedure was developed for synthesis these isocarbostyrils narciclasine (2a) 7-deoxynarciclasine (2c).
A 644-membered library of chalcones was prepared by parallel synthesis using the Claisen−Schmidt base-catalyzed aldol condensation substituted acetophenones and benzaldehydes. The cytotoxicity these conveniently determined upon crude products directly in 96-well microtiter test plates conventional MTT assay. This method revealed seven IC50 less than 1 μM which 4'-hydroxy-2,4,6,3'-tetramethoxychalcone (5a) most active [IC50 (K562), 30 nM]; it causes cell cycle arrest at G2/M point binds to...
Abstract ZL006 and IC87201 have been presented as efficient inhibitors of the nNOS/PSD-95 protein-protein interaction shown great promise in cellular experiments animal models ischemic stroke pain. Here, we investigate proposed mechanism action using biochemical biophysical methods, such fluorescence polarization (FP), isothermal titration calorimetry (ITC) 1 H- 15 N HSQC NMR. Our data show that under applied vitro conditions, do not interact with PDZ domains nNOS or PSD-95, nor inhibit...
The Sudano-Sahelian species Guiera senegalensis J. F. Gmel. is a small shrub found mainly in West Africa. It well known the Sahel, where it grows gregariously, forming abundant single-species colonies on fallow clay or sandy soils. Its widespread use traditional medicine prompted us to conduct an ethnobotanical survey and phytochemical screening of this plant. chemical analysis tests we carried out confirmed results earlier work. main classes secondary metabolites, namely anthraquinones,...
A phthalocyanine–chalcone conjugate has been designed to combine the vascular disrupting effect of chalcones with photodynamic phthalocyanines. This potential dual and antiangiogenic agent was obtained by condensation a tetrahydroxylated non-peripherally substituted Zn(II) phthalocyanine an amino chalcone converted into corresponding activated isocyanate. The fully characterized.