A5081680353- Synthesis and biological activity
- Click Chemistry and Applications
- Synthesis of Organic Compounds
- Chemical Synthesis and Analysis
- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Chemical Synthesis and Reactions
- Synthesis and Biological Activity
- Catalytic Cross-Coupling Reactions
- Protein Degradation and Inhibitors
- Cancer therapeutics and mechanisms
- Synthesis and Biological Evaluation
- Bioactive Compounds and Antitumor Agents
- Monoclonal and Polyclonal Antibodies Research
- Biochemical and Molecular Research
- Glycosylation and Glycoproteins Research
- Synthesis of Indole Derivatives
- Chronic Lymphocytic Leukemia Research
- Multiple Myeloma Research and Treatments
- Coordination Chemistry and Organometallics
- Sulfur-Based Synthesis Techniques
- Organometallic Complex Synthesis and Catalysis
- Organometallic Compounds Synthesis and Characterization
- Plant chemical constituents analysis
- Metal complexes synthesis and properties
Inserm
2013-2023
Aix-Marseille Université
2011-2023
Centre National de la Recherche Scientifique
2013-2023
Institut Paoli-Calmettes
2012-2023
Centre de Recherche en Cancérologie de Marseille
2012-2023
Institut de Biologie Intégrative de la Cellule
2013
Cegep de Saint Jerome
2012
Ludwig-Maximilians-Universität München
2012
Institut National Polytechnique de Toulouse
2011
École Nationale Supérieure Agronomique de Toulouse
2011
To investigate the relation between chemical structure and antimicrobial activity of carvacrol, eugenol, menthol two synthesized carvacrol derivative compounds: methyl ether carvacryl acetate against bacteria, Escherichia coli, Pseudomonas fluorescens, Staphylococcus aureus, Lactobacillus plantarum, Bacillus subtilis, a yeast Saccharomyces cerevisiae one fungi Botrytis cinerea.The was tested in liquid vapour phases, by both broth microatmosphere methods, respectively. The same classification...
A series of A-ring variously methoxylated 4-(3-hydroxy-4-methoxyphenyl)coumarins related to combretastatin A-4 was prepared by cross-coupling reactions. Cytotoxicity studies indicated a potent activity against HBL100 cell line. Substitution patterns on had only slight effect antiproliferative activity. For most cytotoxic compounds, the as potential modulators P-gp and BCRP efflux pumps evaluated. The results show that compounds 2 7 were able restore mitoxantrone accumulation (BCRP) at...
A midthroughput screening follow-up program targeting the first bromodomain of human BRD4 protein, BRD4(BD1), identified an acetylated-mimic xanthine derivative inhibitor. This compound binds with affinity in low micromolar range yet exerts suitable unexpected selectivity vitro against other members and extra-terminal domain (BET) family. structure-based pinpointed a role ZA loop, paving way for development potent selective BET-BRDi probes.
Over the past few decades, hit identification has been greatly facilitated by advances in high-throughput and fragment-based screenings. One major hurdle remaining drug discovery is process automation of hit-to-lead (H2L) optimization. Here, we report a time- cost-efficient integrated strategy for H2L optimization as well partially automated design potent chemical probes consisting focused-chemical-library virtual screening coupled with robotic diversity-oriented de novo synthesis vitro...
Copper-catalyzed O- and N-arylation reactions involving triarylbismuth diacetates or aryllead triacetates are ligand coupling which were discovered in the eighties independently by Bartons Dodonovs groups. These reagents lead generally to efficient arylation under mild neutral conditions (room temperature 40 dgree C, no added basic reagent). Recently, scope of these main group metal mediated was broadened when Chan Evans reported that organoboron compounds can be used as source organic aryl...
A series of A-ring polymethoxylated neoflavonoids was prepared by ligand coupling reactions involving either Suzuki or Stille reactions. Cytotoxicity studies indicated a potent activity against CEM leukemia cell line for the compounds presenting substitution pattern related to that combretastatin A-4. The two having 3'-OH and 4'-OCH3 substituents on 4-phenyl B-ring have no effect human topoisomerases I II but potently inhibit, in vitro, microtubule assembly. At level, active were...
The synthesis of different 4-arylcoumarin analogues combretastatin A-4 led to the identification two new compounds (1 and 2) with potent cytotoxic activity on a CEM leukemia cell line third one completely inactive (compound 3). It was suggested that cytotoxicity 1 2 may be related their interaction microtubules tubulin, since these inhibit microtubule formation from purified tubulin in vitro [Bailly et al. (2003) J. Med. Chem. 46 (25), 5437−5444]. In present study, identified as main target...
A series consisting of ianthelliformisamimes A, B, and C as well its synthetic analogues was prepared in high chemical yield, from 27 to 91%, using peptide coupling the key step, compounds were evaluated for their vitro antibiotic enhancer properties against resistant Gram-negative bacteria clinical isolates. The mechanism action one these derivatives Pseudomonas aeruginosa when combined with doxycycline precisely utilizing bioluminescence measure ATP efflux fluorescence evaluate membrane...
A series of conformationally flexible furan-derived allocolchicinoids was prepared from commercially available colchicine in good to excellent yields using a three-step reaction sequence. Cytotoxicity studies indicated the potent activity two compounds against human epithelial and lymphoid cell lines (AsPC-1, HEK293, Jurkat) as well Wnt-1 related murine line W1308. The results vitro experiments demonstrated that major effect these induction cycle arrest G2/M phase direct consequence...
Over the last 10 years, protein-protein interactions (PPIs) have shown increasing potential as new therapeutic targets. As a consequence, PPIs are today most screened target class in high-throughput screening (HTS). The development of broad chemical libraries dedicated to these particular targets is essential; however, space associated with this 'high-hanging fruit' still under debate. Here, we analyse properties 40 non-redundant small molecules present 2P2I database...
Protein–protein interactions (PPIs) represent an enormous source of opportunity for therapeutic intervention. We and others have recently pinpointed key rules that will help in identifying the next generation innovative drugs to tackle this challenging class targets within decade. used these design oriented chemical library corresponding a set diverse "PPI-like" modulators with cores identified as privileged structures therapeutics. In work, we purchased resulting 1664 structurally compounds...
Cancer cells utilize the main de novo pathway and alternative salvage for deoxyribonucleotide biosynthesis to achieve adequate nucleotide pools. Deoxycytidine kinase is rate-limiting enzyme of it has recently emerged as a target anti-proliferative therapies cancers where essential. Here, we present development potent inhibitor applying an iterative multidisciplinary approach, which relies on computational design coupled with experimental evaluations. This strategy allows acceleration...
Triangular shapes have inspired scientists over time and are common in nature, such as the flower petals of oxalis triangularis, triangular faces tetrahedrite crystals, icosahedron virus capsids. Supramolecular chemistry has enabled construction assemblies, many which possess functional features. Among these structures, cucurbiturils been used to build supramolecular triangles, we recently reported paramagnetic cucurbit[8]uril (CB[8]) but reasons for their formation remain unclear. Several...
2-(methoxymethoxymethyl)aryllead triacetates, obtained in situ from the corresponding arylboronic acids, reacted with 4-hydroxycoumarins, leading to 3-(2-methoxymethoxymethyl)aryl-4-hydroxycoumarin derivatives good high yields. These compounds underwent a cascade sequence of reactions, deprotection-halogenation-annulation, afford polyoxygenated tetracyclic 6H,11H-[2]benzopyrano-[4,3-c] [1]benzopyran-11-ones Some showed moderate cytotoxicity against human epithelial mammary HBL100 cells.
Design of focused chemical libraries dedicated to protein–protein interaction targets.
Masitinib, a highly selective protein kinase inhibitor, can sensitise gemcitabine-refractory cancer cell lines when used in combination with gemcitabine. Here we report reverse proteomic approach that identifies the target responsible for this sensitisation: deoxycytidine (dCK). as well other inhibitors, such imatinib, interact dCK and provoke an unforeseen conformational-dependent activation of nucleoside kinase, modulating phosphorylation analogue drugs. This phenomenon leads to increase...
The synthesis and biological assessment of indole-based allocolchicine congeners with potent anti-proliferative apoptosis-inducing activity are reported.