Search Results - "Tardy, Sébastien"
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In Silico Driven Design and Synthesis of Rhodanine Derivatives as Novel Antibacterials Targeting the Enoyl Reductase InhA
Published in Journal of medicinal chemistry (22-12-2016)“…Here, we report on the design, synthesis, and biological evaluation of 4-thiazolidinone (rhodanine) derivatives targeting Mycobacterial tuberculosis (Mtb)…”
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Discovery of Novel α‑Carboline Inhibitors of the Anaplastic Lymphoma Kinase
Published in ACS omega (24-05-2022)“…The anaplastic lymphoma kinase (ALK) is abnormally expressed and hyperactivated in a number of tumors and represents an ideal therapeutic target. Despite…”
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Study of phenoxy radical couplings using the enzymatic secretome of Botrytis cinerea
Published in Frontiers in chemistry (28-05-2024)“…Phenoxy radical coupling reactions are widely used in nature for the synthesis of complex molecules such as lignin. Their use in the laboratory has great…”
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Novel Mechanism for an Old Drug: Phenazopyridine is a Kinase Inhibitor Affecting Autophagy and Cellular Differentiation
Published in Frontiers in pharmacology (04-08-2021)“…Phenazopyridine is a widely used drug against urinary tract pain. The compound has also been shown to enhance neural differentiation of pluripotent stem cells…”
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Isolation and Identification of Isocoumarin Derivatives With Specific Inhibitory Activity Against Wnt Pathway and Metabolome Characterization of Lasiodiplodia venezuelensis
Published in Frontiers in chemistry (12-08-2021)“…The Wnt signaling pathway controls multiple events during embryonic development of multicellular animals and is carcinogenic when aberrantly activated in…”
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Correction to “Discovery of Novel α‑Carboline Inhibitors of the Anaplastic Lymphoma Kinase”
Published in ACS omega (28-06-2022)Get full text
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From Conception to Development: Investigating PROTACs Features for Improved Cell Permeability and Successful Protein Degradation
Published in Frontiers in chemistry (20-04-2021)“…Proteolysis Targeting Chimeras (PROTACs) are heterobifunctional degraders that specifically eliminate targeted proteins by hijacking the ubiquitin-proteasome…”
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Linkers as Game-changers in PROTAC Technology: Emphasizing General Trends in PROTAC Pharmacokinetics for their Rational Design
Published in Chimia (27-04-2022)“…Proteolysis Targeting Chimeras (PROTACs) are heterobifunctional molecules that act as degraders. They selectively remove disease-associated proteins by…”
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Mammalian RAD52 Functions in Break-Induced Replication Repair of Collapsed DNA Replication Forks
Published in Molecular cell (15-12-2016)“…Human cancers are characterized by the presence of oncogene-induced DNA replication stress (DRS), making them dependent on repair pathways such as…”
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Exploring the Ubiquitin-Proteasome System (UPS) through PROTAC Technology
Published in Chimia (29-04-2020)“…In the context of dysregulated ubiquitylation, the accumulation of oncogenic substrates can lead to tumorigenesis. In particular, mutations in Von…”
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Identification of non-ATP-competitive α-carboline inhibitors of the anaplastic lymphoma kinase
Published in European journal of medicinal chemistry (05-08-2022)“…The Anaplastic Lymphoma Kinase (ALK) is a therapeutic target for personalized medicine in selected cancers. Despite excellent clinical responses to ALK…”
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Regioselective N-vinylation of cyclic thionocarbamates through a vinyl bis-sulfone methodology
Published in Tetrahedron letters (16-08-2004)“…■■■ A vinyl bis-sulfone Michael type approach towards heteroatom vinylation was applied on nitrogen derivatives. Cyclic thionocarbamates––mainly…”
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Synthesis and biological evaluation of benzo[4,5]imidazo[1,2-c]pyrimidine and benzo[4,5]imidazo[1,2-a]pyrazine derivatives as anaplastic lymphoma kinase inhibitors
Published in Bioorganic & medicinal chemistry (15-02-2014)“…Novel fused tricyclic heterocycles were prepared as inhibitors of oncogenic fusion proteins of the ALK tyrosine kinase. The best compound was active against wt…”
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1,3-Oxazoline- and 1,3-oxazolidine-2-thiones as substrates in direct modified Stille and Suzuki cross-coupling
Published in Tetrahedron letters (22-09-2008)“…1,3-Oxazoline- (OXT) and 1,3-oxazolidine-2-thiones (OZT) can undergo direct Stille and Suzuki cross-coupling reactions under microwave activation to produce…”
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Synthesis of Optically Active Monoacid Side-Chains of Cephalotaxus Alkaloids
Published in European Journal of Organic Chemistry (01-01-2009)“…The general preparation of enantiopure monoacid side‐chains of several esters of cephalotaxine is described. The strategy, similar to Weinreb's approach to the…”
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