A5091590853- Synthesis of heterocyclic compounds
- Synthesis and Biological Evaluation
- Phenothiazines and Benzothiazines Synthesis and Activities
- Synthesis and biological activity
- Quinazolinone synthesis and applications
- Effects and risks of endocrine disrupting chemicals
- Synthesis and Characterization of Heterocyclic Compounds
- Pharmacological Receptor Mechanisms and Effects
- Synthesis and Reactivity of Sulfur-Containing Compounds
- Synthesis and Reactions of Organic Compounds
- Toxic Organic Pollutants Impact
- Catalytic Cross-Coupling Reactions
- Synthesis and bioactivity of alkaloids
- Cholinesterase and Neurodegenerative Diseases
- Cancer therapeutics and mechanisms
- Receptor Mechanisms and Signaling
- Catalytic C–H Functionalization Methods
- Chemical synthesis and alkaloids
- Pharmaceutical and Antibiotic Environmental Impacts
- Analytical Chemistry and Chromatography
- Alzheimer's disease research and treatments
- Synthesis and pharmacology of benzodiazepine derivatives
- Free Radicals and Antioxidants
- Computational Drug Discovery Methods
- Chemical Reaction Mechanisms
Université de Poitiers
2017-2024
Centre National de la Recherche Scientifique
2022-2024
Inserm
2017-2024
Centre Hospitalier Universitaire de Poitiers
2018-2023
Écologie et Biologie des Interactions
2021-2023
Université de Lille
2007-2022
Centre Hospitalier Universitaire de Lille
2017-2022
Lille Neurosciences & Cognition
2022
Institut de Chimie des Milieux et des Matériaux de Poitiers
2020
Centre de Recherche Jean Pierre Aubert
2017-2019
The synthesis of novel thiadiazepine derivatives, that could be considered as constraint analogues E-7010, are reported. These molecules were evaluated for their antiproliferative activity toward the murine L1210 leukemia cell line. Flow cytometric studies performed on cells with most cytotoxic compounds showed an accumulation in G2/M phases cycle a significant percentage tetraploid (8N DNA content). Submicromolar cytotoxicities observed 2b, 4b, 4e, 4g, and 4i. Two them, 2b found to potent...
Cancer is a major cause of mortality in developed countries, following only cardiovascular diseases. Death cancerous cells can be achieved by stopping mitosis and the antimitotic class drugs formed spindle poisons used for this purpose. Their role to disorganize mitotic targeting its main constituent, microtubules, themselves made heterodimers alpha beta-tubulin. They disrupt dynamics microtubules either stabilizing them, as do paclitaxel or epothilones, destabilizing colchicine. The binding...
Halogenated BPA (XBPA) forms resulting from water chlorination can lead to increased toxicity and different biological effects. While previous studies have reported the occurrence of XBPAs, analytical limitation hindered analysis differentiation many potential isomeric forms. Using online solid-phase extraction - liquid chromatography ion-mobility high-resolution mass spectrometry (OSPE-LC-IM-HRMS), we demonstrated a rapid method for XBPA after chlorination, with total time less than 10 min...
Three new N1,N5,N10-tris(4-hydroxycinnamoyl)spermidines were isolated from a methanolic root extract of Microdesmis keayana. They identified as N5,N10-di(p-coumaroyl)-N1-feruloylspermidine, N5-(p-coumaroyl)-N1,N10-diferuloylspermidine, and N1,N5,N10-triferuloylspermidine, named keayanidines A, B, C (1–3), respectively. Their structures established by spectral techniques (electrospray mass spectrometry, one- two-dimensional NMR). A 4′,4″,4′′′-trimethylated derivative was prepared methylation...
Background and Purpose Selective agonists of the sigma‐1 receptor (σ1 protein) are generally reported to protect against neuronal damage modulate oligodendrocyte differentiation. Human rodent lymphocytes possess saturable, high‐affinity binding sites for compounds σ1 protein potential immunomodulatory properties have been described ligands. Experimental autoimmune encephalomyelitis ( EAE ) is recognized as a valuable model inflammatory aspects multiple sclerosis MS ). Here, we assessed role...
Halogenated bisphenol A (BPA) derivatives are produced during disinfection treatment of drinking water or synthesized as flame retardants (TCBPA TBBPA). BPA is considered an endocrine disruptor especially on human follicle-stimulating hormone receptor (FSHR). Using a global experimental approach, we assessed the effect halogenated FSHR activity and estimated risk to reproductive health exposed populations. For first time, show that binds derivatives, at 10 nM, concentration lower than those...
A series of new pyridobenzodiazepines with variation the basic side chain were synthesized and evaluated for their binding to D4.2, D2L, 5-HT2A receptors in comparison clozapine, haloperidol, two parent compounds previously described, 8-chloro-6-(4-methyl-1-piperazinyl)-11H-pyrido[2,3-b][1,4]benzodiazepine (8) 8-methyl-6-(4-methyl-1-piperazinyl)-11H-pyrido[2,3-b][1,4]benzodiazepine (9). In piperazine series, replacing N-methyl group by a N-phenyl moiety (15−17, 30−32) provided dramatic...
In order to predict the antioxidant activity of 22 pinoline derivatives (1,2,3,4-tetrahydro-β-carbolines), two dimensional quantitative-structure relationships (2D-QSAR) analysis 19 hexahydropiridoindoles and 12 flavonoids was realized. Five statistically significant models were obtained from randomly constituted training sets (21 compounds) subsquently validated with corresponding test (10 compounds). Antioxidant (pIC50) correlated 5 molecular descriptors calculated software DRAGON. The...