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index medicus (29) 29
humans (17) 17
chemical sciences (16) 16
chemistry, medicinal (15) 15
affinity-chromatography (14) 14
protein kinase inhibitors - chemistry (12) 12
animals (11) 11
immobilized axin (11) 11
organic chemistry (11) 11
protein kinase inhibitors - chemical synthesis (11) 11
protein kinase inhibitors - pharmacology (11) 11
protein-serine-threonine kinases - antagonists & inhibitors (11) 11
dyrk1a (10) 10
structure-activity relationship (10) 10
kinase inhibitors (9) 9
molecular structure (9) 9
phosphorylation (9) 9
[chim]chemical sciences (8) 8
alzheimers-disease (8) 8
life sciences (8) 8
leucettamine b (7) 7
medicinal chemistry (7) 7
microwave-assisted chemistry (7) 7
protein kinases (7) 7
protein-kinases (7) 7
protein-serine-threonine kinases - metabolism (7) 7
protein-tyrosine kinases - antagonists & inhibitors (7) 7
analysis (6) 6
article (6) 6
chemistry, organic (6) 6
derivatives (6) 6
kinase inhibitor (6) 6
[ chim.orga ] chemical sciences/organic chemistry (5) 5
biological evaluation (5) 5
dual-specificity (5) 5
inhibitors (5) 5
mice (5) 5
protein kinase inhibitors - metabolism (5) 5
purification (5) 5
roscovitine (5) 5
alzheimer's disease (4) 4
amines (4) 4
biochemistry & molecular biology (4) 4
chemistry techniques, synthetic (4) 4
ck1 (4) 4
clk (4) 4
clk1 (4) 4
dimroth rearrangement (4) 4
enzyme activation - drug effects (4) 4
phosphotransferases (4) 4
protein kinase inhibitors - therapeutic use (4) 4
protein-serine-threonine kinases - chemistry (4) 4
pyrimidines - chemistry (4) 4
pyrimidines - pharmacology (4) 4
[ chim ] chemical sciences (3) 3
[chim.orga]chemical sciences/organic chemistry (3) 3
alzheimer disease - drug therapy (3) 3
amines - chemical synthesis (3) 3
amines - pharmacology (3) 3
amino acid sequence (3) 3
analogs (3) 3
binding sites (3) 3
biochemistry, molecular biology (3) 3
catalysis (3) 3
cdk5 (3) 3
cell proliferation - drug effects (3) 3
cftr (3) 3
cyclin-dependent kinase (3) 3
cystic fibrosis (3) 3
dimethylformamide (3) 3
dose-response relationship, drug (3) 3
down syndrome (3) 3
drug design (3) 3
drug target (3) 3
efficient synthesis (3) 3
genetics & heredity (3) 3
genomics (3) 3
gsk-3 (3) 3
heterocyclic compounds (3) 3
immune evasion (3) 3
indoles (3) 3
inhibitory concentration 50 (3) 3
kinases (3) 3
molecular docking simulation (3) 3
protein conformation (3) 3
protein-tyrosine kinases - chemistry (3) 3
protein-tyrosine kinases - metabolism (3) 3
proteins (3) 3
pyrimidines - chemical synthesis (3) 3
quinazolines - chemical synthesis (3) 3
quinazolines - chemistry (3) 3
quinazolines - pharmacology (3) 3
trpc6 (3) 3
tyrosine (3) 3
4-f]quinazolin-9-ones (2) 2
4-g]quinazoline (2) 2
[ chim.ther ] chemical sciences/medicinal chemistry (2) 2
[ sdv.bbm ] life sciences [q-bio]/biochemistry, molecular biology (2) 2
[ sdv.mp ] life sciences [q-bio]/microbiology and parasitology (2) 2
adenosine triphosphate - metabolism (2) 2
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1. Full Text Molecular structures of cdc2-like kinases in complex with a new inhibitor chemotype
by Walter, Anne and Chaikuad, Apirat and Helmer, Renate and Loaëc, Nadège and Preu, Lutz and Ott, Ingo and Knapp, Stefan and Meijer, Laurent and Kunick, Conrad
PLoS ONE, ISSN 1932-6203, 05/2018, Volume 13, Issue 5, p. e0196761
Cdc2-like kinases (CLKs) represent a family of serine-threonine kinases involved in the regulation of splicing by phosphorylation of SR-proteins and other... 
CLK1 | RECOGNITION | PHOSPHORYLATION | MULTIDISCIPLINARY SCIENCES | PURIFICATION | SELECTIVE INHIBITORS | DYRK1A | AFFINITY-CHROMATOGRAPHY | DRUG TARGET | SRPK1 INHIBITORS | SPLICING FACTOR | Research | Molecular structure | Protein kinases | Analysis | Cdc2 protein | Phosphorylation | Funding | Genomics | Serine | Selectivity | Kinases | Cancer therapies | Open source software | Proteins | Consortia | Docking | Life sciences | Tyrosine | Threonine | Splicing | Crystallization | Tumor cell lines | Down syndrome | Chromatography | Inhibitors | Cell lines | Splicing factors | Cancer | Pharmaceuticals
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2. Full Text Indole-3-Carbonitriles as DYRK1A Inhibitors by Fragment-Based Drug Design
by Meine, Rosanna and Becker, Walter and Falke, Hannes and Preu, Lutz and Loaëc, Nadège and Meijer, Laurent and Kunick, Conrad
ISSN 1420-3049, 2018
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3. Full Text Indole-3-carbonitriles as DYRK1A inhibitors by fragment-based drug design
by Meine, Rosanna and Becker, Walter and Falke, Hannes and Preu, Lutz and Loaëc, Nadège and Meijer, Laurent and Kunick, Conrad
Molecules, ISSN 1420-3049, 2018, Volume 23, Issue 2, p. 64
Dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) is a potential drug target because of its role in the development of Down syndrome and... 
Fraction of saturation | Fragment-based drug development | Indole | Solubility | DYRK1A | Protein kinase inhibitor | Lipophilicity | Molecular docking | FUNCTIONAL-LINK | indole | ALZHEIMERS-DISEASE | BIOCHEMISTRY & MOLECULAR BIOLOGY | DUAL-SPECIFICITY | CHEMISTRY, MULTIDISCIPLINARY | fraction of saturation | DISCOVERY | INDOLES | MEDICINAL CHEMISTRY | PHOSPHORYLATION-REGULATED KINASES | molecular docking | fragment-based drug development | DOWN-SYNDROME | lipophilicity | protein kinase inhibitor | solubility | LEUCETTAMINE B | PROTEIN-KINASE INHIBITORS | Tyrosine | Cell culture | Phosphorylation | Animal models | Carboxylic acids | Kinases | Assaying | Drug development | Fragmentation | Lipophilic | Inhibitors | Down's syndrome | Quinoline | Chemical synthesis | Cellular structure | Index Medicus
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4. Full Text 10-Iodo-11H‑indolo[3,2‑c]quinoline-6-carboxylic Acids Are Selective Inhibitors of DYRK1A
by Falke, Hannes and Chaikuad, Apirat and Becker, Anja and Loaëc, Nadège and Lozach, Olivier and Abu Jhaisha, Samira and Becker, Walter and Jones, Peter G and Preu, Lutz and Baumann, Knut and Knapp, Stefan and Meijer, Laurent and Kunick, Conrad
Journal of Medicinal Chemistry, ISSN 0022-2623, 04/2015, Volume 58, Issue 7, pp. 3131 - 3143
The protein kinase DYRK1A has been suggested to act as one of the intracellular regulators contributing to neurological alterations found in individuals with... 
Chemistry Techniques, Synthetic | Protein-Tyrosine Kinases - metabolism | Humans | Crystallography, X-Ray | Structure-Activity Relationship | HEK293 Cells - drug effects | Dose-Response Relationship, Drug | Protein Kinase Inhibitors - chemistry | Quinolones - chemistry | Adenosine Triphosphate - metabolism | Carboxylic Acids - chemistry | Protein-Serine-Threonine Kinases - antagonists & inhibitors | Protein-Tyrosine Kinases - chemistry | Protein Conformation | Molecular Docking Simulation | Protein Kinase Inhibitors - pharmacology | Protein-Serine-Threonine Kinases - chemistry | Binding Sites | Indoles - chemistry | Protein-Serine-Threonine Kinases - metabolism | Protein Kinase Inhibitors - metabolism | Protein-Tyrosine Kinases - antagonists & inhibitors | Index Medicus
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5. Full Text TRPC6 channel translocation into phagosomal membrane augments phagosomal function
by Vladimir Riazanski and Aida G. Gabdoulkhakova and Lin S. Boynton and Raphael R. Eguchi and Ludmila V. Deriy and D. Kyle Hogarth and Nadège Loaëc and Nassima Oumata and Hervé Galons and Mary E. Brown and Pavel Shevchenko and Alexander J. Gallan and Sang Gune Yoo and Anjaparavanda P. Naren and Mitchel L. Villereal and Daniel W. Beacham and Vytautas P. Bindokas and Lutz Birnbaumer and Laurent Meijer and Deborah J. Nelson
Proceedings of the National Academy of Sciences of the United States of America, ISSN 0027-8424, 11/2015, Volume 112, Issue 47, pp. E6486 - E6495
Defects in the innate immune system in the lung with attendant bacterial infections contribute to lung tissue damage, respiratory insufficiency, and ultimately... 
Roscovitine | Cystic fibrosis | TRPC6 | Phagosome | Alveolar macrophage | CELLS | alveolar macrophage | PHAGOCYTOSIS | RESPIRATORY-DISEASE | MULTIDISCIPLINARY SCIENCES | ACIDIFICATION | IDENTIFICATION | DRUG TARGETS | roscovitine | cystic fibrosis | LIPID RAFTS | phagosome | ALVEOLAR MACROPHAGES | CYSTIC-FIBROSIS | CFTR | Small Molecule Libraries - pharmacology | Receptors, G-Protein-Coupled - metabolism | Calcium - metabolism | Humans | Protein Transport - drug effects | Acids - metabolism | Exocytosis - drug effects | Diglycerides - metabolism | Cell Membrane - metabolism | Cell Membrane - drug effects | Pertussis Toxin - pharmacology | Phagosomes - drug effects | Cell Line | TRPC6 Cation Channel | Microbial Viability - drug effects | Purines - pharmacology | Phagosomes - metabolism | Cystic Fibrosis Transmembrane Conductance Regulator - metabolism | Small Molecule Libraries - chemistry | Patch-Clamp Techniques | Animals | Purines - chemistry | Calcium Signaling - drug effects | Macrophages, Alveolar - drug effects | Models, Biological | Fluorescent Antibody Technique | TRPC Cation Channels - metabolism | Intracellular Membranes - drug effects | Mice | Macrophages, Alveolar - metabolism | Intracellular Membranes - metabolism | Ion Channel Gating - drug effects | Phagocytes | Immune response | Translocation (Genetics) | Genetic research | Ion channels | Genetic aspects | Research | Properties | Biological Sciences | PNAS Plus
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6. Full Text Design and synthesis of thiazolo[5,4-f]quinazolines as DYRK1A inhibitors, part I
by Foucourt, Alicia and Hédou, Damien and Dubouilh-Benard, Carole and Désiré, Laurent and Casagrande, Anne-Sophie and Leblond, Bertrand and Loäec, Nadège and Meijer, Laurent and Besson, Thierry
Molecules, ISSN 1420-3049, 10/2014, Volume 19, Issue 10, pp. 15546 - 15571
The convenient synthesis of a library of novel 6,6,5-tricyclic thiazolo[5,4-f]quinazolines (forty molecules) was achieved mainly under microwave irradiation.... 
Kinases inhibitors | GSK3α/β | Microwave-assisted chemistry | DYRK1A | Dimroth rearrangement | Thiazolo[5,4-f]quinazolines | Appel salt | microwave-assisted chemistry | GSK3 alpha/beta | ALZHEIMERS-DISEASE | DRUG DISCOVERY | EFFICIENT SYNTHESIS | CHEMISTRY, ORGANIC | KINASE INHIBITORS | kinases inhibitors | PROTEIN-KINASES | appel salt | BIOLOGICAL EVALUATION | AFFINITY-CHROMATOGRAPHY | thiazolo[5,4-f]quinazolines | LEUCETTAMINE B | IMMOBILIZED AXIN | MULTISTEP SYNTHESIS | Quinazolines - chemical synthesis | Protein Kinase Inhibitors - chemical synthesis | Chemistry Techniques, Synthetic | Humans | Structure-Activity Relationship | Protein Kinase Inhibitors - chemistry | Drug Design | Protein-Serine-Threonine Kinases - antagonists & inhibitors | Protein-Tyrosine Kinases - chemistry | Thiazoles | Inhibitory Concentration 50 | Molecular Structure | Protein Kinase Inhibitors - pharmacology | Protein-Serine-Threonine Kinases - chemistry | Quinazolines - pharmacology | Quinazolines - chemistry | Protein-Tyrosine Kinases - antagonists & inhibitors | Chemical Sciences
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7. Full Text Marine-derived 2-aminoimidazolone alkaloids. Leucettamine B-related polyandrocarpamines inhibit mammalian and protozoan DYRK & CLK kinases
by Loaëc, Nadège and Attanasio, Eletta and Villiers, Beno t and Durieu, Emilie and Tahtouh, Tania and Cam, Morgane and Davis, Rohan A and Alencar, Aline and Roué, Mélanie and Bourguet-Kondracki, Marie-Lise and Proksch, Peter and Limanton, Emmanuelle and Guiheneuf, Solène and Carreaux, Fran ois and Bazureau, Jean-Pierre and Klautau, Michelle and Meijer, Laurent
Marine Drugs, ISSN 1660-3397, 10/2017, Volume 15, Issue 10, p. 316
A large diversity of 2-aminoimidazolone alkaloids is produced by various marine invertebrates, especially by the marine Calcareous sponges Leucetta and... 
CLK | Alzheimer’s disease | 2-aminoimidazolone alkaloids | Marine sponge | Polyandrocarpamines | Down syndrome | Kinase inhibitor | DYRK | Leucettine | Ascidian | Calcarea | Porifera | Polyandrocarpa | Protein kinases | Leucettamine B | HYMENIALDISINE | leucettine | CYCLIN D1 | protein kinases | marine sponge | BENZYLIDENE 2-AMINOIMIDAZOLONES | AFFINITY-CHROMATOGRAPHY | Alzheimer's disease | IMMOBILIZED AXIN | CHEMISTRY, MEDICINAL | NATURAL-PRODUCTS | RECEPTOR ANTAGONIST | ascidian | kinase inhibitor | SPONGE ALKALOIDS | polyandrocarpamines | LEUCETTINE L41 | leucettamine B | IMIDAZOLE ALKALOIDS | Phosphorylation | Protozoan Proteins - antagonists & inhibitors | Humans | Imidazoles - chemistry | Alkaloids - chemical synthesis | Structure-Activity Relationship | Phylogeny | Protozoan Infections - drug therapy | Amines - therapeutic use | Protein-Serine-Threonine Kinases - antagonists & inhibitors | Antiprotozoal Agents - chemical synthesis | Imidazoles - chemical synthesis | Imidazoles - therapeutic use | Porifera - chemistry | Protein Kinase Inhibitors - chemical synthesis | Alkaloids - pharmacology | Alzheimer Disease - drug therapy | Imidazoles - pharmacology | Amines - chemical synthesis | Antiprotozoal Agents - pharmacology | Porifera - genetics | Animals | Protein Kinase Inhibitors - therapeutic use | Down Syndrome - drug therapy | Alkaloids - therapeutic use | Protein Kinase Inhibitors - pharmacology | Antiprotozoal Agents - therapeutic use | Amines - pharmacology | Urochordata - chemistry | Protein-Tyrosine Kinases - antagonists & inhibitors | Drugs | Cdc2 protein | Disease | Cyclin D1 | Drug development | Kinases | Proteins | Alkaloids | Marine invertebrates | Microorganisms | Specificity | Plankton | Down's syndrome | Tyrosine | Medical treatment | Sponges | Pharmacology | Mammals | Cells | Diseases | Inhibitors | Reviews | Invertebrates | Chemical Sciences
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8. Full Text Correction of cognitive deficits in mouse models of Down syndrome by a pharmacological inhibitor of DYRK1A
by Nguyen, Thu Lan and Nguyen, Thu Lan and Duchon, Arnaud and Duchon, Arnaud and Manousopoulou, Antigoni and Manousopoulou, Antigoni and Loaëc, Nadège and Loaëc, Nadège and Villiers, Benoît and Villiers, Benoit and Pani, Guillaume and Pani, Guillaume and Karatas, Meltem and Karatas, Meltem and Mechling, Anna E and Harsan, Laura-Adela and Harsan, Laura-Adela and Limanton, Emmanuelle and Limanton, Emmanuelle and Bazureau, Jean-Pierre and Bazureau, Jean-Pierre and Carreaux, François and Carreaux, François and Garbis, Spiros D and Garbis, Spiros D and Meijer, Laurent and Meijer, Laurent and Herault, Yann and Herault, Yann
Disease models & mechanisms, ISSN 1754-8403, 09/2018, Volume 11, Issue 9, p. dmm035634
Growing evidence supports the implication of DYRK1A in the development of cognitive deficits seen in Down syndrome (DS) and Alzheimer's disease (AD). We here... 
Leucettine | DYRK1A | Down syndrome | Synapsin | Kinase inhibitor | FUNCTIONAL CONNECTIVITY | BINDING-PROTEIN | DUAL-SPECIFICITY | PATHOLOGY | MICROTUBULE DYNAMICS | CELL BIOLOGY | INTELLECTUAL DISABILITY | TRANSMITTER RELEASE | REGULATED KINASE 1A | SYNDROME CRITICAL REGION | INCREASED DOSAGE | SYNAPSIN-I | Dioxoles - therapeutic use | Phosphorylation | Protein-Tyrosine Kinases - metabolism | Imidazoles - chemistry | Cytoplasm - metabolism | Nerve Net - drug effects | RNA, Messenger - metabolism | Synapsins - metabolism | Protein Kinase Inhibitors - chemistry | Protein-Tyrosine Kinases - genetics | Synapses - metabolism | Protein Binding - drug effects | Protein-Serine-Threonine Kinases - antagonists & inhibitors | Dioxoles - pharmacology | Down Syndrome - complications | Cognitive Dysfunction - complications | Imidazoles - therapeutic use | Nerve Net - physiopathology | Protein-Serine-Threonine Kinases - metabolism | Disease Models, Animal | Cognitive Dysfunction - drug therapy | Amino Acid Sequence | Down Syndrome - pathology | Synapses - drug effects | Biocatalysis | Brain - physiopathology | Mice, Inbred C57BL | RNA, Messenger - genetics | Protein-Serine-Threonine Kinases - genetics | Imidazoles - pharmacology | Cognitive Dysfunction - pathology | Dioxoles - chemistry | Synapsins - chemistry | Brain - drug effects | Magnetic Resonance Imaging | Animals | Protein Kinase Inhibitors - therapeutic use | Proteomics | Brain - pathology | Cytoskeleton - metabolism | Mice | Mice, Inbred BALB C | Protein Kinase Inhibitors - pharmacology | Cytoskeleton - drug effects | Protein-Tyrosine Kinases - antagonists & inhibitors | Chemical Sciences | 302
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9. Full Text Novel adociaquinone derivatives from the Indonesian sponge Xestospongia sp
by He, Fei and Mai, Linh H and Longeon, Arlette and Copp, Brent R and Loaëc, Nadège and Bescond, Amandine and Meijer, Laurent and Bourguet-Kondracki, Marie-Lise
Marine Drugs, ISSN 1660-3397, 05/2015, Volume 13, Issue 5, pp. 2617 - 2628
Seven new adociaquinone derivatives, xestoadociaquinones A (1a), B (1b), 14-carboxy-xestoquinol sulfate (2) and xestoadociaminals A-D (3a, 3c, 4a, 4c),... 
Adociaquinone | Xestoadociaquinone | 14-carboxy-xestoquinol sulfate | Xestospongia sp | Kinase inhibitor | Xestoadociaminal | kinase inhibitor | SAPRA | CHEMISTRY, MEDICINAL | HALENAQUINONE DERIVATIVES | XESTOQUINONE | xestoadociaquinone | xestoadociaminal | INHIBITORS | adociaquinone | MARINE SPONGE | Animals | Magnetic Resonance Spectroscopy - methods | Antioxidants - chemistry | Anti-Bacterial Agents - chemistry | Bacteria - drug effects | Protein Kinases - chemistry | Naphthoquinones - chemistry | Naphthoquinones - pharmacology | Cell Proliferation - drug effects | Xestospongia - chemistry | Porifera - chemistry
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10. Full Text Synthesis, Resolution, and Biological Evaluation of Atropisomeric (aR)- and (aS)‑16-Methyllamellarins N: Unique Effects of the Axial Chirality on the Selectivity of Protein Kinases Inhibition
by Yoshida, Kenyu and Itoyama, Ryosuke and Yamahira, Masashi and Tanaka, Junji and Loaëc, Nadège and Lozach, Olivier and Durieu, Emilie and Fukuda, Tsutomu and Ishibashi, Fumito and Meijer, Laurent and Iwao, Masatomo
Journal of Medicinal Chemistry, ISSN 0022-2623, 09/2013, Volume 56, Issue 18, pp. 7289 - 7301
The total synthesis of the optically active (aR)- and (aS)-16-methyllamellarins N (3a and 3b) was achieved via resolution on HPLC chiral stationary phase. The... 
CYCLIN-DEPENDENT KINASES | CHEMISTRY, MEDICINAL | PHARMACOLOGICAL INHIBITORS | ANALOGS | DRUG DISCOVERY | PURIFICATION | LAMELLARIN-ALPHA 20-SULFATE | TOPOISOMERASE-I | AFFINITY-CHROMATOGRAPHY | IMMOBILIZED AXIN | ALKALOIDS | Protein Kinases - metabolism | Topoisomerase I Inhibitors - metabolism | Polycyclic Compounds - chemical synthesis | Stereoisomerism | Antineoplastic Agents - chemical synthesis | Humans | DNA Topoisomerases, Type I - chemistry | Protein Kinases - chemistry | Substrate Specificity | Structure-Activity Relationship | Antineoplastic Agents - metabolism | Protein Kinase Inhibitors - chemistry | Topoisomerase I Inhibitors - pharmacology | Antineoplastic Agents - pharmacology | Polycyclic Compounds - metabolism | Topoisomerase I Inhibitors - chemistry | Polycyclic Compounds - chemistry | Protein Kinase Inhibitors - chemical synthesis | Chemistry Techniques, Synthetic | DNA Topoisomerases, Type I - metabolism | Antineoplastic Agents - chemistry | Polycyclic Compounds - pharmacology | Topoisomerase I Inhibitors - chemical synthesis | Cell Line, Tumor | Protein Conformation | Molecular Docking Simulation | Protein Kinase Inhibitors - pharmacology | Protein Kinase Inhibitors - metabolism
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11. Full Text Exploration of the imidazo[1,2-b]pyridazine scaffold as a protein kinase inhibitor
by Bendjeddou, Lyamin Z and Loaëc, Nadège and Villiers, Benoît and Prina, Eric and Späth, Gerald F and Galons, Hervé and Meijer, Laurent and Oumata, Nassima
European Journal of Medicinal Chemistry, ISSN 0223-5234, 01/2017, Volume 125, pp. 696 - 709
3,6-Disubstituted imidazo[1,2-b]pyridazine derivatives were synthesized to identify new inhibitors of various eukaryotic kinases, including mammalian and... 
Leishmania, DYRK1A | Unicellular parasites | Kinase inhibitor | Imidazo[1,2-b]pyridazine | CLKs | CHEMISTRY, MEDICINAL | CLK | 1 PFCDPK1 | PHOSPHORYLATION | DYRK1A | DUAL-SPECIFICITY | DISCOVERY | POTENT | IMIDAZOPYRIDAZINES | LEUCETTAMINE B | DERIVATIVES | Cell Survival - drug effects | Protein Kinase Inhibitors - chemical synthesis | Pyridazines - pharmacology | Enzyme Activation - drug effects | Pyridazines - chemical synthesis | Pyridazines - chemistry | Antiparasitic Agents - chemical synthesis | Protein Kinase Inhibitors - chemistry | Antiparasitic Agents - pharmacology | Inhibitory Concentration 50 | Eukaryota - drug effects | Molecular Structure | Protein Kinase Inhibitors - pharmacology | Antiparasitic Agents - chemistry | Malaria | Plasmodium falciparum | Protein kinases | Index Medicus | Life Sciences | Microbiology and Parasitology
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12. Full Text 9- and 11-substituted 4-azapaullones are potent and selective inhibitors of African trypanosoma
by Maiwald, Franziska and Benítez, Diego and Charquero, Diego and Dar, Mahin Abad and Erdmann, Hanna and Preu, Lutz and Koch, Oliver and Hölscher, Christoph and Loaëc, Nadège and Meijer, Laurent and Comini, Marcelo A and Kunick, Conrad
European Journal of Medicinal Chemistry, ISSN 0223-5234, 08/2014, Volume 83, pp. 274 - 283
Trypanosomes from the “brucei” complex are pathogenic parasites endemic in sub-Saharan Africa and causative agents of severe diseases in humans and livestock.... 
Nagana | Chalcones | Cinnamides | Trypanosoma brucei brucei | Paullones | Human trypanosomiasis | CHEMISTRY, MEDICINAL | VALIDATION | BRUCEI | HUMAN SERUM | SIDE-CHAINS | TRYPANOTHIONE SYNTHETASE | BLOOD-STREAM | AFFINITY-CHROMATOGRAPHY | DRUG TARGET | IMMOBILIZED AXIN | Cell Line | Humans | Trypanocidal Agents - toxicity | Trypanocidal Agents - chemistry | Structure-Activity Relationship | Benzazepines - pharmacology | Benzazepines - chemical synthesis | Trypanosoma brucei brucei - drug effects | Trypanosoma brucei brucei - physiology | Trypanosomiasis, African - parasitology | Animals | Trypanocidal Agents - pharmacology | Drug Design | Trypanocidal Agents - chemical synthesis | Macrophages - drug effects | Cell Proliferation - drug effects | Mice | Benzazepines - toxicity | Benzazepines - chemistry | Substitution reactions | Antiparasitic agents | Livestock | Trypanocidal Agents/chemistry | Trypanocidal Agents/chemical synthesis | Trypanosoma brucei brucei/drug effects | Trypanocidal Agents/pharmacology | Biochemistry, Molecular Biology | Benzazepines/pharmacology | Trypanosomiasis, African/parasitology | Life Sciences | Benzazepines/toxicity | Macrophages/drug effects | Benzazepines/chemistry | Trypanosoma brucei brucei/physiology | Trypanocidal Agents/toxicity | Cell Proliferation/drug effects | Benzazepines/chemical synthesis
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13. Full Text Acridone Alkaloids from Glycosmis chlorosperma as DYRK1A Inhibitors
by Beniddir, Mehdi A and Le Borgne, Erell and Iorga, Bogdan I and Loaëc, Nadège and Lozach, Olivier and Meijer, Laurent and Awang, Khalijah and Litaudon, Marc
Journal of Natural Products, ISSN 0163-3864, 05/2014, Volume 77, Issue 5, pp. 1117 - 1122
Two new acridone alkaloids, chlorospermines A and B (1 and 2), were isolated from the stem bark of Glycosmis chlorosperma, together with the known... 
CHEMISTRY, MEDICINAL | PHOSPHORYLATION | KINASE INHIBITORS | SULFUR-CONTAINING AMIDES | PROTEIN-KINASES | PLANT SCIENCES | CHEMICAL-CONSTITUENTS | CDK1/CYCLIN B | PHARMACOLOGY & PHARMACY | AFFINITY-CHROMATOGRAPHY | LEUCETTAMINE B | IMMOBILIZED AXIN | PENTAPHYLLA | Acridones - chemistry | Alkaloids - isolation & purification | Protein-Serine-Threonine Kinases - antagonists & inhibitors | Nuclear Magnetic Resonance, Biomolecular | Malaysia | Molecular Structure | Rutaceae - chemistry | Acridones - isolation & purification | Alkaloids - chemistry | Protein-Tyrosine Kinases - antagonists & inhibitors | Chemical Sciences
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14. Full Text Synthesis and biological evaluation of N-aryl-7-methoxybenzo[b]furo[3,2-d]pyrimidin-4-amines and their N-arylbenzo[b]thieno[3,2-d]pyrimidin-4-amine analogues as dual inhibitors of CLK1 and DYRK1A kinases
by Loidreau, Yvonnick and Marchand, Pascal and Dubouilh-Benard, Carole and Nourrisson, Marie-Renée and Duflos, Muriel and Loaëc, Nadège and Meijer, Laurent and Besson, Thierry
European Journal of Medicinal Chemistry, ISSN 0223-5234, 01/2013, Volume 59, pp. 283 - 295
Novel -aryl-7-methoxybenzo[ ]furo[3,2- ]pyrimidin-4-amines ( ) and their -arylbenzo[ ]thieno[3,2- ]pyrimidin-4-amine analogues ( ) were designed and prepared... 
CLK | Microwave-assisted chemistry | Benzo[b]furo[3,2-d]pyrimidin-4-amines | Kinase inhibitors | Alzheimer's disease | Benzo[b]thieno[3,2-d]pyrimidin-4-amines | DYRK | CHEMISTRY, MEDICINAL | DECOMPOSITION | PROTEIN-KINASES | LEUCETTINES | CONVENIENT ROUTE | FORMAMIDE | PURIFICATION | DISEASE | TARGETS | AFFINITY-CHROMATOGRAPHY | DERIVATIVES | Amines - chemistry | Pyrimidines - chemical synthesis | Furans - pharmacology | Humans | Enzyme Inhibitors - pharmacology | Thiophenes - pharmacology | Amines - chemical synthesis | Pyrimidines - pharmacology | Enzyme Activation - drug effects | Pyrimidines - chemistry | Thiophenes - chemical synthesis | Furans - chemistry | Protein-Serine-Threonine Kinases - antagonists & inhibitors | Inhibitory Concentration 50 | Molecular Structure | Furans - chemical synthesis | Thiophenes - chemistry | Amines - pharmacology | Protein-Tyrosine Kinases - antagonists & inhibitors | Amines | Dimethylformamide | Heterocyclic compounds | Phosphotransferases | Analysis | Organic chemistry | Chemical Sciences
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15. Full Text Synthesis and preliminary in vitro kinase inhibition evaluation of new diversely substituted pyrido[3,4-g]quinazoline derivatives
by Zeinyeh, Wael and Esvan, Yannick J and Nauton, Lionel and Loaëc, Nadège and Meijer, Laurent and Théry, Vincent and Anizon, Fabrice and Giraud, Francis and Moreau, Pascale
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 09/2016, Volume 26, Issue 17, pp. 4327 - 4329
(10 μM): 96% CDK5 inhibition, 98% GSK3 inhibition. Docking models of into CDK5 (A) and GSK3 (B) ATP-binding sites. The synthesis of new diversely substituted... 
CLK1 | Protein kinase inhibition | CDK5 | GSK3 | DYRK1A | CK1 | Pyrido[3,4-g]quinazoline | CHEMISTRY, MEDICINAL | CHEMISTRY, ORGANIC | Quinazolines - chemical synthesis | Protein Kinase Inhibitors - chemical synthesis | Pyridines - chemistry | Nitro Compounds - chemistry | Pyridines - chemical synthesis | Protein-Tyrosine Kinases - classification | Enzyme Activation - drug effects | Protein Kinase Inhibitors - chemistry | Protein Kinase Inhibitors - pharmacology | Pyridines - pharmacology | Quinazolines - pharmacology | Binding Sites | Quinazolines - chemistry | Protein-Tyrosine Kinases - antagonists & inhibitors | Analysis | Resveratrol | Chemical Sciences
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16. Full Text Synthesis and molecular modelling studies of 8-arylpyrido[3',2':4,5thieno[3,2-d]pyrimidin-4-amines as multitarget Ser/Thr kinases inhibitors
by Loidreau, Yvonnick and Deau, Emmanuel and Marchand, Pascal and Nourrisson, Marie-Renée and Logé, Cédric and Coadou, Gaël and Loaëc, Nadège and Meijer, Laurent and Besson, Thierry
European Journal of Medicinal Chemistry, ISSN 0223-5234, 2015, Volume 92, pp. 124 - 134
This paper reports the design and synthesis of a novel series of 8-arylpyrido[3′,2′:4,5]thieno[3,2-d]pyrimidin-4-amines via microwave-assisted multi-step... 
Medicinal Chemistry | Organic chemistry | Chemical Sciences
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17. Full Text Synthesis and biological evaluation of N-arylbenzo[b]thieno[3,2-d]pyrimidin-4-amines and their pyrido and pyrazino analogues as Ser/Thr kinase inhibitors
by Loidreau, Yvonnick and Marchand, Pascal and Dubouilh-Benard, Carole and Nourrisson, Marie-Renée and Duflos, Muriel and Lozach, Olivier and Loaëc, Nadège and Meijer, Laurent and Besson, Thierry
European Journal of Medicinal Chemistry, ISSN 0223-5234, 12/2012, Volume 58, pp. 171 - 183
A useful and rapid access to libraries of -arylbenzo[ ]thieno[3,2- ]pyrimidin-4-amines and their pyrido and pyrazino analogues was designed and optimized for... 
Thieno[3,2-d]pyrimidine | Dimroth rearrangement | Kinase inhibitor | Alzheimer's disease | Microwave-assisted chemistry | Dimethylformamide dimethylacetal | CHEMISTRY, MEDICINAL | ALZHEIMERS-DISEASE | EFFICIENT SYNTHESIS | DECOMPOSITION | MICROWAVE IRRADIATION | PROTEIN-KINASES | FACTOR RECEPTOR EGFR | FORMAMIDE | AFFINITY-CHROMATOGRAPHY | DERIVATIVES | IMMOBILIZED AXIN | Protein Kinase Inhibitors - chemical synthesis | Pyrimidines - chemical synthesis | Humans | Rats | Thiophenes - pharmacology | Structure-Activity Relationship | Pyrimidines - pharmacology | Pyrimidines - chemistry | Dose-Response Relationship, Drug | Pyrazines - chemistry | Thiophenes - chemical synthesis | Protein Kinase Inhibitors - chemistry | Animals | Swine | Protein-Serine-Threonine Kinases - antagonists & inhibitors | Molecular Structure | Protein Kinase Inhibitors - pharmacology | Pyridones - chemistry |