Search Results - "Combes, Sebastien"
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CRCM5484: A BET-BDII Selective Compound with Differential Anti-leukemic Drug Modulation
Published in Journal of medicinal chemistry (14-04-2022)“…Differentially screening the Fr-PPIChem chemical library on the bromodomain and extra-terminal (BET) BRD4-BDII versus -BDI bromodomains led to the discovery of…”
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Triangular Regulation of Cucurbit[8]uril 1:1 Complexes
Published in Journal of the American Chemical Society (10-04-2019)“…Triangular shapes have inspired scientists over time and are common in nature, such as the flower petals of oxalis triangularis, the triangular faces of…”
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3
New Ianthelliformisamine Derivatives as Antibiotic Enhancers against Resistant Gram-Negative Bacteria
Published in Journal of medicinal chemistry (22-05-2014)“…A series consisting of ianthelliformisamimes A, B, and C as well as its synthetic analogues was prepared in high chemical yield, from 27 to 91%, using peptide…”
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Synthesis and Biological Evaluation of 4-Arylcoumarin Analogues of Combretastatins. Part 2
Published in Journal of medicinal chemistry (12-05-2011)“…A series of A-ring variously methoxylated 4-(3-hydroxy-4-methoxyphenyl)coumarins related to combretastatin A-4 was prepared by cross-coupling reactions…”
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First evidence for the use of polyamines as nucleophiles in a regioselective palladium-catalyzed allylic amination reaction
Published in Tetrahedron (23-12-2014)“…Palladium-catalyzed reaction of unsymmetrical allylic electrophiles with polyamines gives rise to regioisomeric allylic polyamines. An original catalytic…”
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Synthesis and antiprotozoal activity of 4-arylcoumarins
Published in European journal of medicinal chemistry (01-03-2010)“…A large series of 4-arylcoumarins was synthesized by Suzuki-Miyaura cross-coupling reaction and evaluated for antiprotozoal activity against Plasmodium…”
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Allocolchicinoids bearing a Michael acceptor fragment for possible irreversible binding of tubulin
Published in RSC medicinal chemistry (01-06-2020)“…We describe an attempt to apply the concept of covalent binding towards the highly active allocolchicinoids selected on the basis of SAR analysis of previously…”
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The indolylcoumarin COUFIN exhibits potent activity against renal carcinoma cells without affecting hematopoietic system
Published in Anti-cancer agents in medicinal chemistry (01-01-2014)“…The present work describes the anticancer activity of a new indolylcoumarin named COUFIN and more specifically, its efficiency against clear cell renal…”
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Synthesis and biological evaluation of polymethoxylated 4-heteroarylcoumarins as tubulin assembly inhibitor
Published in Bioorganic & medicinal chemistry (01-10-2008)“…A series of syn-restricted polymethoxylated 4-heteroarylcoumarins—the isostuctural analogs of combretastatin A-4—was synthesized by Suzuki–Miyaura…”
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Synthesis and biological evaluation of novel anticancer bivalent colchicine–tubulizine hybrids
Published in Bioorganic & medicinal chemistry (15-07-2012)“…A series of novel antimitotic hybrids were synthesized in good yields by linking of azide-containing colchicine congeners with acetylene-substituted…”
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Dinitroxides for Solid State Dynamic Nuclear Polarization
Published in Applied magnetic resonance (01-07-2012)“…We have prepared a series of dinitroxides and we investigated their properties as polarizing agents for solid-state nuclear magnetic resonance/dynamic nuclear…”
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Interaction of 4-Arylcoumarin Analogues of Combretastatins with Microtubule Network of HBL100 Cells and Binding to Tubulin
Published in Biochemistry (Easton) (01-08-2006)“…The synthesis of different 4-arylcoumarin analogues of combretastatin A-4 led to the identification of two new compounds (1 and 2) with potent cytotoxic…”
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Tumor selective cytotoxic action of a thiomorpholin hydroxamate inhibitor (TMI-1) in breast cancer
Published in PloS one (18-09-2012)“…Targeted therapies, associated with standard chemotherapies, have improved breast cancer care. However, primary and acquired resistances are frequently…”
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Hot water treatments reduce leaf yellowing and extend vase life of Asiatic hybrid lilies
Published in Postharvest biology and technology (01-02-2012)“…► Short duration hot water treatment (HWT) of the leaves of Asiatic lilies can effectively minimise leaf yellowing in stored, and non-stored stems. ► Reduction…”
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4-Arylcoumarin analogues of combretastatins stimulate apoptosis of leukemic cells from chronic lymphocytic leukemia patients
Published in Experimental hematology (01-12-2008)“…Objective To investigate the proapoptotic capacities of four arylcoumarin analogues of combretastatins on leukemic cells from B-cell chronic lymphocytic…”
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Integrated Strategy for Lead Optimization Based on Fragment Growing: The Diversity-Oriented-Target-Focused-Synthesis Approach
Published in Journal of medicinal chemistry (12-07-2018)“…Over the past few decades, hit identification has been greatly facilitated by advances in high-throughput and fragment-based screenings. One major hurdle…”
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Exploring Selective Inhibition of the First Bromodomain of the Human Bromodomain and Extra-terminal Domain (BET) Proteins
Published in Journal of medicinal chemistry (25-02-2016)“…A midthroughput screening follow-up program targeting the first bromodomain of the human BRD4 protein, BRD4(BD1), identified an acetylated-mimic xanthine…”
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Cascade Synthesis of Polyoxygenated 6H,11H-[2]Benzopyrano-[4,3-c][1]benzopyran-11-ones
Published in Journal of organic chemistry (27-04-2007)“…2-(Methoxymethoxymethyl)aryllead triacetates, obtained in situ from the corresponding arylboronic acids, reacted with 4-hydroxycoumarins, leading to…”
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From a drug repositioning to a structure-based drug design approach to tackle acute lymphoblastic leukemia
Published in Nature communications (29-05-2023)“…Cancer cells utilize the main de novo pathway and the alternative salvage pathway for deoxyribonucleotide biosynthesis to achieve adequate nucleotide pools…”
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A clickable melphalan for monitoring DNA interstrand crosslink accumulation and detecting ICL repair defects in Fanconi anemia patient cells
Published in Nucleic acids research (25-08-2023)“…Abstract Fanconi anemia (FA) is a genetic disorder associated with developmental defects, bone marrow failure and cancer. The FA pathway is crucial for the…”
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