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Catalytic fluorination of chlorinated aromatic compounds : Synthesis of fluorinated building blocks for agrochemecal and pharmacochemical applications. – FLUORCAT
This work deals with the gas phase catalysed fluorination of chloropyridines using metal fluorides as catalysts and HF as fluorination agent. Indeed, until now, these fluorinated molecules, used as building blocks for the preparation of more complex molecules with therapeutic applications and / or
A key enzyme in nucleic acid biosynthesis : The 5’-cytosolic nucleotidase (cN-II) as new drug target – cN-II Focus
Nucleoside analogues are widely used as therapeutic agents, especially to treat leukemia and solid tumors. Their use is somehow limited by the appearance of resistance mechanims, with multifactorial origins and still not fully understand. Thus, recent works indicated that these mechanisms mainly con
The timescales of disorder in proteins – DYN-IDP
It is clear that many proteins execute essential biological functions with no well-defined 3D-structure. This is in direct contradiction to Pauling’s rule, which states that a functional protein should necessarily have a well-defined three-dimensional fold. Intrinsically disordered proteins (IDPs) c
Flexible Molecular Plateform, a Tool for Catalysis – P2MOC
In a particularly competitive international context, the objectives are to associate several catalytic concepts and/or to generate multiple activations using a unique family of polyfonctional promoters.The general motif of this family includes a pyridine and a pendant methylamine arm. Development o
Catalytic C(sp3)-H bond functionalization of enolates – EnolFun
This fundamental research project is positioned in a frontier field of organic synthesis and organometallic catalysis. Its main goal is the development of new methods for the direct functionalization of alkyl groups of organic molecules by organopalladium catalysis, via the chemistry of enolates. Th
Total Synthesis of amphidinolides C, C2 et F: Potant marine natural products in the anticancer therapy. – AMPHICTOT
The natural products have always been a pool of drug or drug-candidates. In particular in the cancer treatment, important molecules were discovered from nature. The most famous examples in France are taxoids and Vinca alkaloids, isolated from the yew and Madagascar periwinkle respectively (Taxol and
New approach to aqueous biphasic catalysis through catalyst confinement in nanoscopic core-shell polymers – BIPHASNANOCAT
This project is included in the wider framework of green chemistry, meaning the search by chemists to provide society with safer chemical fabrication, using the minimum amount of ldangerous and toxic reagents, using as little energy as possible, producing the minimum possible waste… To achieve thes
New hybrid metalloprotein catalysts for selective oxidation by dioxygen. – CATHYMETOXY
To catalyse oxidation reactions in sustainable conditions is a challenge which cannot be solved using conventional approaches. The combination of additional know-how is irequired. The last 20 years allowed to clarify the crucial role of biomolecules to catalyse oxidation reactions, to better underst
Discovery of new chemoselective ligation reactions by High Throughput Screening – ClickScreen
The goal of the clickscreen project is to identify among thousands of parallel reactions conducted by mixing reactive functions with metals those displaying high efficiency and selectivity. Thanks to a powerfull screening method developed by the lab, thousands of reactions trials can be evaluated in
Assembly/disassembly of innovative prodrug systems using click-unclick strategy – Click-unclick
The goal of this project is to develop novel nanosystems allowing the release of an active substance at a specific target organ. The strategy aims at trigger the release of the drug with light. The drug can be linked to a peptide carrier or embeded within mesoporous nanoparticles. The development of
Kinetically-tunable self-immolative aromatic spacers – KITUSE
Self-immolative spacers are already used in prodrug strategies. Our aim was to accurately control the self-immolation rate. The measurements of the rate of this type of reaction were made possible by a construction involving a step of rapid photoactivation; most previous works were based on a slow e
Designing HOst Materials for high-efficiency Electrophosphorescent Organic Light Emitting Diodes: A new approach – HOME-OLED
In order to reduce domestic and public energy consumption, new efficient sources of low-energy white light are urgently required. The development of Phosphorescent OLEDs using host-guest emitting layers has led to numerous efficient green and red Phosphorescent OLEDs. However, the lack of effective
Inhibitors for Bacterial Efflux Pumps – IBEF
In Gram-negative bacteria, the over-expression of efflux pumps (EP) is involved in the Multi-Drug Resistance phenotype (MDR). EPs recognize a large panel of substrates including all antibiotic and biocide families. These EPs favor the acquisition of additional resistance mechanisms such as target mu
Antibiofilm surface treatment with dendrimer/Copper multilayers – COPPERTREE
Bacterial colonies grow on many surfaces. These biofilms are present in evaporation towers of nuclear power plants or on the submerged part of ship hulls. They are sometimes resistant to conventional antibacterial treatments, and can be the cause of serious infections when developing on implants or
Total Synthesis of Mirabalin isomers and Simplified analogs – STIMAS
Mirabaline has been isolated in small quantities from a marine sponge. From its antitumoral activity and the complexity of its structure, this molecule is synthetically attractive. One goal is to synthesize mirabalin, 4 isomers and 4 simplified analogues to determine the exact structure of mirabali
Quadrupolar carbo-chromophores and alpha-graphyne – Carbo-ChromMat
Polyacetylenic molecules are today studied not only for their aesthetic appearance, but also for their promising physical properties and related applications, notably in optical devices highlighting their non-linear optical (NLO) properties such as the two-photon absorption (2PA). Two types of targ
Remote B-H activation in unconventional multidentate boranes. – ReBAB
ReBAB deals with the design and the study of the coordination of unconventional polyfunctional boranes L~BHR in order to understand the different factors that promote the B-H activation through a remote control strategy involving a functional group distant from the B-H bond.In this domain, the state
Organocatalyzed Enantioselective REactions with Keto Amides – OEREKA
cf doc en provenance de l'ANR cf doc en provenance de l'ANR cf doc en provenance de l'ANR cf doc en provenance de l'ANR The project OEREKA focuses on the development of original and synthetically useful methodologies in the field of organocatalysis and multiple bond-forming transformations (MBFTs),
Oligo-arylamide mimics of double stranded DNA – ARYNAMICS
Nucleic acids (NAs) play a central role among biomolecular processes. A key property of NAs is their involvement in innumerable interactions with proteins through their surface features, i.e. their overall shape, the array of phosphate ions and the chemical groups belonging to bases that are expose
Operando study in temperature and pressure of the conversion of syngas loaded with typical impurities derived from biomass to methane and higher hydrocarbons. – BioSyngOp
This project addresses crucial technological problems related to the utilisation of synthesis gas derived from biomass gasification (biosyngas: mixture of CO, CO2, H2 and impurities), thus pertaining to the wider societal agendas dealing with global warming and local production of cheap and sustaina
Design of artificial metalloenzymes by functional mutation of proteins : access to new enantioselective catalysts – ARTZYMES
At the industrial level, important synthons are obtained via biocatalytic processes involving whole microorganisms or isolated enzymes. In particular, these processes offer an efficient access to chiral molecules under mild, environmentally-friendly conditions. However, the repertoire of reactions c
Development of new eco-aware asymmetric catalytic processes; Photocatalyzed oxidation with water as the unique oxygen atom source. – Water Act
The necessary surch for new energies has stimulated researchers to design new photocatalysts. In the course of the development of new, eco-aware catalytic systems and to achieve efficient asymmetric catalytic oxygenation of organic substrates, we were interested in the design of a photocatalyst comb
Molecules combining C60 and iminosugars: synthesis and multivalent effects on glycosidases inhibition – Sweet60s
The main objective of the Sweet60s project is to provide a clear understanding of the significant inhibition enhancements observed for glycosidases with multivalent iminosugars. A better understanding of the multivalent effect for enzyme inhibition in general and the establishment of structure/prope
An Alternative Design for Chiral Brønsted Acid Organocatalysts – CHIRACID
Catalysis offers the prospect of efficient synthetic routes to chemical products, i.e. pharmaceuticals as well as agrochemicals and materials. After the unquestionable success of enzymatic, heterogeneous and homogeneous transition metal catalysis, in the past decade attention has been focused on org
ORGANOMETALLIC LIGANDS: A NEW STRATEGY TO CONSTRUCT LUMINESCENT ASSEMBLIES FOR OPTOELECTRONICS – OPTOELECTR-OM
Coordination complexes of iridium(III), ruthenium(II), platinum(II) and gold(III) with phenylpyridyl and polypyridyl chelating ligands constitute an important class of chromophores because of their unique photophysical properties. As a consequent such compounds, especially iridium(III), platinum(II)
Modulation of Integrase Activity by Means of Conformationaly Constrained Nucleotides – MIAM CoCoNuts
Can we modulate the protein tendency to recognise its DNA partner by imposing to the latter the structure it should adopt at the final stage of the complex? Is substrate preorganization able to lead to a new inhibitor class or at least to define a novel strategy for protein activity modulation? Alph
Hybrid organic-inorganic polyoxometalates with biological and optical properties – BIOOPOM
The first part of the project consisted in the synthesis of hybrid polyoxometalates (POMs) containing bisphosphonate (BP) ligands for their anticancer properties. POMs have been known for a long time for their biological activity while BPs are a class of molecules widely used in the treatment of ost
New Free-radical Multicomponent Processes – RAD-MCR
Our project is part of the current concern of organic chemists to follow in their work the 12 principles of the so-called «green« chemistry, an innovative concept dealing comprehensively with the problem of pollution control. Our research program concerns the development of new, environmentally frie
Large Alkaline-Earths : From Fundamental Organometallic Chemistry to Green Catalysis – GreenLAkE
This project revolves around (i) the organometallic chemistry of large alkalino-earth elements (Ae: calcium, strontium and barium) and (ii) the design of efficient, well-defined catalysts based on such metal centers, to promote highly atom-efficient reactions, namely ring-opening polymerization (ROP
The chemistry of carbene-borane and carbene-silane complexes – NHCX
This project seeks to introduce non toxic reagents for organic and polymer synthesis that are derived from abundant sources not applicable at that stage This project seeks to introduce non toxic reagents for organic and polymer synthesis that are derived from abundant sources 3 publications 1) «[
Structure-function relationships of Ferric Uptake Regulators and their inhibitors: towards new peptido-siderophore antibacterial compounds – PepSiFUR
Iron homeostasis and virulence of pathogens are intimately linked. A key actor of this metabolism in bacteria is the Fur protein (Ferric uptake regulator), a global transcriptional regulator of the expression of the genes involved in iron homeostasis. Any perturbation of Fur activity will affect pro
Total synthesis of 13-desmethyl spirolide C – SPIROSYN
Spirolides produced by dinoflagellates are toxic to marine animals and humans leading to health and economic problems. The muscarinic and nicotinic receptors of the central nervous system are supposed to be their targets. The development of the total synthesis of the original 13-desmethylspirolide C
Polyfonctional Oxaprolines: Asymmetric Synthesis via 1,3-Dipolar Cycloaddition, Evaluation as New Organocatalysts and as Precursors of Disubstituted and Constrained Aminoacids – OXAPROL
Amino acids are ubiquitous molecules in Nature, as they are the major building blocks of proteins. Moreover, in the last 15 years, amino acids such as proline and its derivatives have emerged as potent catalysts to promote biomimetic chemical reactions. In both these fields, the developpement of nov