Laurent Meijer

Laurent Meijer

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Laurent Meijer

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Long-Term Fipronil Treatment Induces Hyperactivity in Female Mice.

Int J Environ Res Public Health 2020 02 29;17(5). Epub 2020 Feb 29.

Perha Pharmaceuticals & ManRos Therapeutics, Centre de Perharidy, 29680 Roscoff, Bretagne, France.

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http://dx.doi.org/10.3390/ijerph17051579DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7084594PMC
February 2020

[]-Annulated Halogen-Substituted Indoles as Potential DYRK1A Inhibitors.

Molecules 2019 Nov 13;24(22). Epub 2019 Nov 13.

Institut für Medizinische und Pharmazeutische Chemie, Technische Universität Braunschweig, Beethovenstraße 55, 38106 Braunschweig, Germany.

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http://dx.doi.org/10.3390/molecules24224090DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6891749PMC
November 2019

A Collection of Bioactive Nitrogen-Containing Molecules from the Marine Sponge .

Mar Drugs 2019 Aug 15;17(8). Epub 2019 Aug 15.

Laboratoire Molécules de Communication et Adaptation des Micro-organismes, UMR 7245 CNRS, Muséum National d'Histoire Naturelle, 57 rue Cuvier (C.P. 54), 75005 Paris, France.

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http://dx.doi.org/10.3390/md17080472DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6723059PMC
August 2019

Structural analogues of roscovitine rescue the intracellular traffic and the function of ER-retained ABCB4 variants in cell models.

Sci Rep 2019 04 30;9(1):6653. Epub 2019 Apr 30.

Inserm, Sorbonne Université, Centre de Recherche Saint-Antoine (CRSA), UMR_S 938, Institute of Cardiometabolism and Nutrition (ICAN), F-75012, Paris, France.

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http://dx.doi.org/10.1038/s41598-019-43111-yDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6491434PMC
April 2019

A facile consensus ranking approach enhances virtual screening robustness and identifies a cell-active DYRK1α inhibitor.

Future Med Chem 2018 10 16;10(20):2411-2430. Epub 2018 Oct 16.

Department of Pharmaceutical Chemistry, School of Pharmacy, University of Athens, Panepistimiopolis Zografou, 157 71 Athens, Greece.

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https://www.future-science.com/doi/10.4155/fmc-2018-0198
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http://dx.doi.org/10.4155/fmc-2018-0198DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6479281PMC
October 2018

Molecular structures of cdc2-like kinases in complex with a new inhibitor chemotype.

PLoS One 2018 3;13(5):e0196761. Epub 2018 May 3.

Institut für Medizinische und Pharmazeutische Chemie, Technische Universität Braunschweig, Braunschweig, Germany.

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http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0196761PLOS
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5933782PMC
August 2018

Harnessing Neutrophil Survival Mechanisms during Chronic Infection by : Novel Therapeutic Targets to Dampen Inflammation in Cystic Fibrosis.

Front Cell Infect Microbiol 2017 30;7:243. Epub 2017 Jun 30.

Institut National de la Santé et de la Recherche Médicale, U1016, Institut CochinParis, France.

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http://dx.doi.org/10.3389/fcimb.2017.00243DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5492487PMC
March 2018

Genetic and pharmacological inhibition of Cdk1 provides neuroprotection towards ischemic neuronal death.

Cell Death Discov 2018 16;4:43. Epub 2018 Mar 16.

1Laboratory of Developmental Neurobiology, GIGA-Neurosciences, University of Liège, C.H.U. B36, 4000 Liège, Belgium.

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http://dx.doi.org/10.1038/s41420-018-0044-7DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5856839PMC
March 2018

Indole-3-Carbonitriles as DYRK1A Inhibitors by Fragment-Based Drug Design.

Molecules 2018 Jan 24;23(2). Epub 2018 Jan 24.

Institut für Medizinische und Pharmazeutische Chemie, Technische Universität Braunschweig, Beethovenstraße 55, 38106 Braunschweig, Germany.

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http://dx.doi.org/10.3390/molecules23020064DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6017736PMC
January 2018

Dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) inhibitors: a survey of recent patent literature.

Expert Opin Ther Pat 2017 Nov 2;27(11):1183-1199. Epub 2017 Aug 2.

f Normandie Univ , UNIROUEN, INSA Rouen, CNRS, COBRA UMR 6014 , Rouen , France.

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http://dx.doi.org/10.1080/13543776.2017.1360285DOI Listing
November 2017

Identification of CLK1 Inhibitors by a Fragment-linking Based Virtual Screening.

Mol Inform 2017 04 21;36(4). Epub 2016 Dec 21.

Technische Universität Dortmund, Fakultät für Chemie und chemische Biologie, Otto-Hahn-Straße 6, 44227, Dortmund, Germany.

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http://dx.doi.org/10.1002/minf.201600123DOI Listing
April 2017

Exploration of the imidazo[1,2-b]pyridazine scaffold as a protein kinase inhibitor.

Eur J Med Chem 2017 Jan 22;125:696-709. Epub 2016 Sep 22.

ManRos Therapeutics, Perharidy Research Center, 29680 Roscoff, Bretagne, France. Electronic address:

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http://dx.doi.org/10.1016/j.ejmech.2016.09.064DOI Listing
January 2017

Further investigation of Paprotrain: Towards the conception of selective and multi-targeted CNS kinase inhibitors.

Eur J Med Chem 2016 Nov 31;124:920-934. Epub 2016 Aug 31.

Centre de Recherche de Gif, Institut de Chimie des Substances Naturelles, CNRS, 1 Avenue de la Terrasse, 91198, Gif-sur-Yvette, France. Electronic address:

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http://dx.doi.org/10.1016/j.ejmech.2016.08.069DOI Listing
November 2016

Chloromethylhalicyclamine B, a Marine-Derived Protein Kinase CK1δ/ε Inhibitor.

J Nat Prod 2016 11 9;79(11):2953-2960. Epub 2016 Nov 9.

The NeaNat Group, Dipartimento di Farmacia, Università degli Studi di Napoli Federico II , Via D. Montesano 49, 80131 Napoli, Italy.

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http://dx.doi.org/10.1021/acs.jnatprod.6b00939DOI Listing
November 2016

Synthesis and preliminary in vitro kinase inhibition evaluation of new diversely substituted pyrido[3,4-g]quinazoline derivatives.

Bioorg Med Chem Lett 2016 09 16;26(17):4327-9. Epub 2016 Jul 16.

Université Clermont Auvergne, Université Blaise Pascal, Institut de Chimie de Clermont-Ferrand, BP 10448, F-63000 Clermont-Ferrand, France; CNRS, UMR 6296, ICCF, F-63178 Aubière, France. Electronic address:

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http://dx.doi.org/10.1016/j.bmcl.2016.07.032DOI Listing
September 2016

Discovery of pyrido[3,4-g]quinazoline derivatives as CMGC family protein kinase inhibitors: Design, synthesis, inhibitory potency and X-ray co-crystal structure.

Eur J Med Chem 2016 Aug 5;118:170-7. Epub 2016 Apr 5.

Université Clermont Auvergne, Université Blaise Pascal, Institut de Chimie de Clermont-Ferrand, BP 10448, F-63000 Clermont-Ferrand, France; CNRS, UMR 6296, ICCF, F-63178 Aubière, France. Electronic address:

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http://dx.doi.org/10.1016/j.ejmech.2016.04.004DOI Listing
August 2016

5-Substituted 3-chlorokenpaullone derivatives are potent inhibitors of Trypanosoma brucei bloodstream forms.

Bioorg Med Chem 2016 08 13;24(16):3790-800. Epub 2016 Jun 13.

Technische Universität Braunschweig, Institut für Medizinische und Pharmazeutische Chemie, Beethovenstraße 55, D-38106 Braunschweig, Germany; Technische Universität Braunschweig, Center of Pharmaceutical Engineering (PVZ), Franz-Liszt-Straße 35A, D-38106 Braunschweig, Germany. Electronic address:

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https://linkinghub.elsevier.com/retrieve/pii/S09680896163044
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http://dx.doi.org/10.1016/j.bmc.2016.06.023DOI Listing
August 2016

Novel optimization of valmerins (tetrahydropyrido[1,2-a]isoindolones) as potent dual CDK5/GSK3 inhibitors.

Eur J Med Chem 2016 Jun 2;115:311-25. Epub 2016 Mar 2.

Institut de Chimie Organique et Analytique, Université d'Orléans, UMR CNRS 7311, Rue de Chartres, BP 6759, 45067, Orléans Cedex 2, France. Electronic address:

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http://dx.doi.org/10.1016/j.ejmech.2016.02.072DOI Listing
June 2016

Synthesis of Thiazolo[5,4-f]quinazolin-9(8H)-ones as Multi-Target Directed Ligands of Ser/Thr Kinases.

Molecules 2016 Apr 30;21(5). Epub 2016 Apr 30.

Normandie Univ; Uni Rouen; INSA; CNRS, COBRA, UMR 6014, 76000 Rouen, France.

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http://dx.doi.org/10.3390/molecules21050578DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6273584PMC
April 2016

Aβ-42 lowering agents from the marine-derived fungus Dichotomomyces cejpii.

Steroids 2015 Dec 9;104:182-8. Epub 2015 Oct 9.

Institute for Pharmaceutical Biology, University of Bonn, 53115 Bonn, Germany. Electronic address:

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https://linkinghub.elsevier.com/retrieve/pii/S0039128X150025
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http://dx.doi.org/10.1016/j.steroids.2015.09.012DOI Listing
December 2015

Advances in tetrahydropyrido[1,2-a]isoindolone (valmerins) series: Potent glycogen synthase kinase 3 and cyclin dependent kinase 5 inhibitors.

Eur J Med Chem 2015 Aug 27;101:274-87. Epub 2015 Jun 27.

Univ Orleans, CNRS UMR 7311, Institut de Chimie Organique et Analytique, rue de Chartres, BP 6759, 45067 Orléans Cedex 2, France. Electronic address:

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http://dx.doi.org/10.1016/j.ejmech.2015.06.046DOI Listing
August 2015

Antitumoral effects of cyclin-dependent kinases inhibitors CR8 and MR4 on chronic myeloid leukemia cell lines.

J Biomed Sci 2015 Jul 17;22:57. Epub 2015 Jul 17.

Laboratoire de Thérapie Cellulaire et Immunobiologie du Cancer, Université de Bretagne Occidentale, CHRU Morvan, 5 avenue Foch, 29609, Brest Cedex, France.

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http://dx.doi.org/10.1186/s12929-015-0163-xDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4504225PMC
July 2015

10-iodo-11H-indolo[3,2-c]quinoline-6-carboxylic acids are selective inhibitors of DYRK1A.

J Med Chem 2015 Apr 23;58(7):3131-43. Epub 2015 Mar 23.

†Institut für Medizinische und Pharmazeutische Chemie, Technische Universität Braunschweig, Beethovenstraße 55, 38106 Braunschweig, Germany.

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http://dx.doi.org/10.1021/jm501994dDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4506206PMC
April 2015

Novel Adociaquinone Derivatives from the Indonesian Sponge Xestospongia sp.

Mar Drugs 2015 Apr 28;13(5):2617-28. Epub 2015 Apr 28.

Laboratoire Molécules de Communication et Adaptation des Micro-organismes, CNRS/MNHN 7245, Muséum National d'Histoire Naturelle, 57 rue Cuvier (C.P. 54), 75005 Paris, France.

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http://dx.doi.org/10.3390/md13052617DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4446597PMC
April 2015

Synthesis and molecular modelling studies of 8-arylpyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-amines as multitarget Ser/Thr kinases inhibitors.

Eur J Med Chem 2015 Mar 23;92:124-34. Epub 2014 Dec 23.

Normandie Univ, COBRA, UMR 6014 & FR 3038; Univ Rouen; INSA Rouen; CNRS, Bâtiment IRCOF, 1 rue Tesnière, 76821 Mont St Aignan Cedex, France. Electronic address:

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http://dx.doi.org/10.1016/j.ejmech.2014.12.038DOI Listing
March 2015

Dispacamide E and other bioactive bromopyrrole alkaloids from two Indonesian marine sponges of the genus Stylissa.

Nat Prod Res 2015 Feb 12;29(3):231-8. Epub 2014 Aug 12.

a Institutfür Pharmazeutische Biologie und Biotechnologie, Heinrich-Heine Universität , Geb. 26.23, Universitätsstrasse 1, D-40225 Düsseldorf , Germany.

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http://dx.doi.org/10.1080/14786419.2014.947496DOI Listing
February 2015

Impact of meriolins, a new class of cyclin-dependent kinase inhibitors, on malignant glioma proliferation and neo-angiogenesis.

Neuro Oncol 2014 Nov 2;16(11):1484-98. Epub 2014 Jun 2.

Inserm U982, Laboratory of Neuronal and Neuroendocrine Communication and Differentiation, Astrocyte and Vascular Niche, Biomedical Research Institute (IRIB), PRES Normandy, TC2N network, University of Rouen, Mont-Saint-Aignan, France (M.J., C.L., L.D., M.-T.S., V.L., P.G., H.C.); Neuro-oncology department, Hospices Civils de Lyon, Hôpital Neurologique, Bron, France (C.M., J.H.); Lyon Neuroscience Research Center INSERM U1028/CNRS UMR 5292, Lyon, France (C.M., J.H.); University of Claude Bernard - Lyon 1, Villeurbanne, France (C.M., J.H.); Institut de Chimie et Biochimie Moléculaires et Supramoléculaires UMR 5246, University of Claude Bernard - Lyon 1, Villeurbanne, France (F.L., G.L., B.J., N.L.); Protein Phosphorylation & Human Disease Group & USR3151, Station Biologique, Roscoff, France (N.L., L.M.); ManRos Therapeutics, Roscoff, France (L.M.).

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http://dx.doi.org/10.1093/neuonc/nou102DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4201071PMC
November 2014

Synthesis of new pyridazino[4,5-b]indol-4-ones and pyridazin-3(2H)-one analogs as DYRK1A inhibitors.

Bioorg Med Chem Lett 2014 Nov 16;24(21):5037-40. Epub 2014 Sep 16.

Université de Nantes, Nantes Atlantique Universités, Laboratoire de Chimie Thérapeutique, Cibles et Médicaments des Infections et du Cancer, IICIMED-EA 1155, UFR Sciences Pharmaceutiques, 1 rue Gaston Veil, Nantes F-44035 Cedex 1, France.

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http://dx.doi.org/10.1016/j.bmcl.2014.09.017DOI Listing
November 2014

The pleiotropic profile of the indirubin derivative 6BIO overcomes TRAIL resistance in cancer.

Biochem Pharmacol 2014 Sep 25;91(2):157-67. Epub 2014 Jul 25.

Pharmaceutical Biology, Department of Pharmacy-Center for Drug Research, Ludwig-Maximilians-University, Butenandtstr. 5-13, 81377 Munich, Germany.

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http://dx.doi.org/10.1016/j.bcp.2014.07.009DOI Listing
September 2014

Several human cyclin-dependent kinase inhibitors, structurally related to roscovitine, are new anti-malarial agents.

Molecules 2014 Sep 23;19(9):15237-57. Epub 2014 Sep 23.

Laboratoire de Chimie et Biochimie Pharmacologiques et Toxicologiques (LCBPT), UMR 8601 CNRS, Université Paris Descartes, Sorbonne Paris Cité, UFR Biomédicale des Saints Pères, 45 rue des Saints-Pères, Paris 75270, France.

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http://dx.doi.org/10.3390/molecules190915237DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6271241PMC
September 2014

Design and synthesis of thiazolo[5,4-f]quinazolines as DYRK1A inhibitors, part I.

Molecules 2014 Sep 29;19(10):15546-71. Epub 2014 Sep 29.

Normandie Université, Laboratoire C.O.B.R.A., UMR 6014 and FR 3038; Université de Rouen; INSA de Rouen; CNRS, Bâtiment I.R.C.O.F. rue Tesnière, Mont-Saint-Aignan F-76821, France.

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http://dx.doi.org/10.3390/molecules191015546DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6270991PMC
September 2014

9- and 11-Substituted 4-azapaullones are potent and selective inhibitors of African trypanosoma.

Eur J Med Chem 2014 Aug 11;83:274-83. Epub 2014 Jun 11.

Technische Universität Braunschweig, Institut für Medizinische und Pharmazeutische Chemie, Beethovenstraße 55, D-38106 Braunschweig, Germany. Electronic address:

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http://dx.doi.org/10.1016/j.ejmech.2014.06.020DOI Listing
August 2014

Synthesis and biological evaluation of tetrahydro[1,4]diazepino[1,2-a]indol-1-ones as cyclin-dependent kinase inhibitors.

Eur J Med Chem 2014 Aug 28;83:617-29. Epub 2014 Jun 28.

Institut de Chimie et Biochimie Moléculaires et Supramoléculaires UMR CNRS 5246, Université de Lyon, Université Claude Bernard - Lyon 1, Bâtiment Curien, 43 Boulevard du 11 novembre 1918, F-69622 Villeurbanne, France. Electronic address:

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http://dx.doi.org/10.1016/j.ejmech.2014.06.063DOI Listing
August 2014

Synthesis and optimization of an original V-shaped collection of 4-7-disubstituted pyrido[3,2-d]pyrimidines as CDK5 and DYRK1A inhibitors.

Eur J Med Chem 2014 Jun 22;80:352-63. Epub 2014 Apr 22.

Institut de Chimie Organique et Analytique, CNRS UMR 7311, B.P. 6759, 45067 Orléans Cedex 2, France. Electronic address:

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http://dx.doi.org/10.1016/j.ejmech.2014.04.055DOI Listing
June 2014

New 5-ylidene rhodanine derivatives based on the dispacamide A model.

Mol Divers 2014 May 2;18(2):375-88. Epub 2014 Mar 2.

Université de Rennes 1 Institut des Sciences Chimiques de Rennes ISCR UMR CNRS 6226, groupe Ingénierie Chimique et Molécules pour le Vivant (ICMV), Bât. 10 A, Campus de Beaulieu, CS 74205, 263 Avenue du Général Leclerc, 35042,  Rennes Cedex, France.

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http://dx.doi.org/10.1007/s11030-014-9509-7DOI Listing
May 2014

Acridone alkaloids from Glycosmis chlorosperma as DYRK1A inhibitors.

J Nat Prod 2014 May 5;77(5):1117-22. Epub 2014 May 5.

Centre de Recherche de Gif, Institut de Chimie des Substances Naturelles, CNRS, LabEx CEBA , 1, Avenue de la Terrasse, 91198 Gif-sur-Yvette Cedex, France.

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http://dx.doi.org/10.1021/np400856hDOI Listing
May 2014

cdc-like/dual-specificity tyrosine phosphorylation-regulated kinases inhibitor leucettine L41 induces mTOR-dependent autophagy: implication for Alzheimer's disease.

Mol Pharmacol 2014 Mar 23;85(3):441-50. Epub 2013 Dec 23.

Centre National de la Recherche Scientifique (CNRS), USR3151, "Protein Phosphorylation and Human Disease," Station Biologique, Roscoff cedex, France (X.F., E.D.); Institut National de la Santé et de la Recherche Médicale/Université Paul Sabatier Unité Mixte de Recherche (UMR) 1048, "Production et fonctions plaquettaires: signalisation et phosphoinositides" group, Institut des Maladies Métaboliques et Cardiovasculaires (I2MC), Toulouse cedex, France (G.C., B.P.); Department of Physiology, Wayne State University School of Medicine, Detroit, Michigan (D.S., A.S.); Laboratoire Sciences Chimiques de Rennes, UMR CNRS 6226, Groupe Ingénierie Chimique et Molécules pour le Vivant (ICMV), Université de Rennes, Campus de Beaulieu, Rennes cedex, France (E.L., F.C., J.-P.B.); and ManRos Therapeutics, Perharidy Research Center, Roscoff, Bretagne, France (L.M.).

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http://dx.doi.org/10.1124/mol.113.090837DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6067634PMC
March 2014

Synthesis, biological evaluation and molecular modelling studies of 4-anilinoquinazoline derivatives as protein kinase inhibitors.

Bioorg Med Chem 2014 Mar 31;22(6):1909-15. Epub 2014 Jan 31.

School of Pharmaceutical Sciences, Rajiv Gandhi Proudyogiki Vishwavidyalaya, Airport Bypass Road, Gandhi Nagar, Bhopal (MP) 462036, India. Electronic address:

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http://dx.doi.org/10.1016/j.bmc.2014.01.044DOI Listing
March 2014

[Search for natural substances with therapeutic activity: George R. Pettit].

Med Sci (Paris) 2014 Mar 31;30(3):319-28. Epub 2014 Mar 31.

Association « Jardin de plantes anticancéreuses », place de l'Évêché, 29250 Saint-Pol-de-Léon, France - ManRos Therapeutics, centre de Perharidy, 29680 Roscoff, France.

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http://www.medecinesciences.org/10.1051/medsci/20143003021
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http://dx.doi.org/10.1051/medsci/20143003021DOI Listing
March 2014

Targeting cyclin-dependent kinases in anti-neoplastic therapy.

Curr Opin Cell Biol 2013 Dec 6;25(6):772-9. Epub 2013 Sep 6.

ManRos Therapeutics, Centre de Perharidy, 29680 Roscoff, France.

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http://dx.doi.org/10.1016/j.ceb.2013.08.004DOI Listing
December 2013

Synthesis of novel 7-substituted pyrido[2',3':4,5]furo[3,2-d]pyrimidin-4-amines and their N-aryl analogues and evaluation of their inhibitory activity against Ser/Thr kinases.

Bioorg Med Chem Lett 2013 Dec 17;23(24):6784-8. Epub 2013 Oct 17.

Normandie Univ, COBRA, UMR 6014 & FR 3038; Univ Rouen; INSA Rouen; CNRS, Bâtiment IRCOF, 1 rue Tesnière, 76821 Mont St Aignan Cedex, France.

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http://dx.doi.org/10.1016/j.bmcl.2013.10.019DOI Listing
December 2013

CDK10/cyclin M is a protein kinase that controls ETS2 degradation and is deficient in STAR syndrome.

Proc Natl Acad Sci U S A 2013 Nov 11;110(48):19525-30. Epub 2013 Nov 11.

P2I2 Group, Protein Phosphorylation and Human Disease Unit, Station Biologique, Centre National de la Recherche Scientifique (CNRS), Unité de Service et de Recherche USR3151, 29680 Roscoff, France.

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http://dx.doi.org/10.1073/pnas.1306814110DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3845122PMC
November 2013

Indirubin derivative 6BIO suppresses metastasis.

Cancer Res 2013 Oct 14;73(19):6004-12. Epub 2013 Aug 14.

Authors' Affiliations: Pharmaceutical Biology, Department of Pharmacy, University of Munich, Munich, Germany; and Centre Nationale de la Recherche Scientifique, Station Biologique, Roscoff, France.

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http://dx.doi.org/10.1158/0008-5472.CAN-12-4358DOI Listing
October 2013

A western blot assay to measure cyclin dependent kinase activity in cells or in vitro without the use of radioisotopes.

FEBS Lett 2013 Sep 15;587(18):3089-95. Epub 2013 Aug 15.

Cancer Cell Laboratory, Department of Biological Sciences, University of Lethbridge, 4401 University Dr, Lethbridge, AB T1K 3M4, Canada.

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http://dx.doi.org/10.1016/j.febslet.2013.08.003DOI Listing
September 2013

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.

J Med Chem 2013 Sep 13;56(18):7289-301. Epub 2013 Sep 13.

Division of Chemistry and Materials Sciences, Graduate School of Engineering, Nagasaki University , 1-14 Bunkyo-machi, Nagasaki 852-8521, Japan.

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http://dx.doi.org/10.1021/jm400719yDOI Listing
September 2013

Pharmacokinetics and biodistribution of the cyclin-dependent kinase inhibitor -CR8- in mice.

BMC Pharmacol Toxicol 2013 Sep 30;14:50. Epub 2013 Sep 30.

Experimental Cancer Medicine (ECM), Laboratory Medicine, Karolinska Institutet, 141 86, Stockholm, Sweden.

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http://dx.doi.org/10.1186/2050-6511-14-50DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3849647PMC
September 2013

Cyclin-dependent kinase inhibitors closer to market launch?

Expert Opin Ther Pat 2013 Aug 22;23(8):945-63. Epub 2013 Apr 22.

Laboratoire de Chimie Organique 2, INSERM U 1022, Université Paris - Descartes, 4 avenue de l'Observatoire, 75270 Paris cedex 06, France.

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http://dx.doi.org/10.1517/13543776.2013.789861DOI Listing
August 2013

Chemical synthesis and biological validation of immobilized protein kinase inhibitory Leucettines.

Eur J Med Chem 2013 Apr 6;62:728-37. Epub 2013 Feb 6.

Université de Rennes 1, Institut des Sciences Chimiques de Rennes, ISCR UMR CNRS 6226, Groupe Ingénierie Chimique & Molécules pour le Vivant (ICMV), Bât. 10A, Campus de Beaulieu, Avenue du Général Leclerc, CS 74205, 35042 Rennes cedex, Bretagne, France.

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http://dx.doi.org/10.1016/j.ejmech.2013.01.035DOI Listing
April 2013

Natural aristolactams and aporphine alkaloids as inhibitors of CDK1/cyclin B and DYRK1A.

Molecules 2013 Mar 6;18(3):3018-27. Epub 2013 Mar 6.

Centre de Recherche de Gif, Institut de Chimie des Substances Naturelles, CNRS, 1 avenue de la Terrasse, 91198 Gif-sur-Yvette Cedex, France.

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http://dx.doi.org/10.3390/molecules18033018DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6269938PMC
March 2013

Potent inhibitors of CDK5 derived from roscovitine: synthesis, biological evaluation and molecular modelling.

Bioorg Med Chem Lett 2013 Jan 10;23(1):125-31. Epub 2012 Nov 10.

Laboratoire de Chimie et Biochimie Pharmacologiques et Toxicologiques, UMR 8601 CNRS, Université Paris Descartes, Sorbonne Paris Cité, UFR Biomédicale des Saints Pères, 45 rue des Saints Pères, 75270 Paris cedex 06, France.

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http://dx.doi.org/10.1016/j.bmcl.2012.10.141DOI Listing
January 2013

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.

Eur J Med Chem 2013 Jan 24;59:283-95. Epub 2012 Nov 24.

Université de Rouen, Laboratoire de Chimie Organique et Bio-organique, Réactivité et Analyse (C.O.B.R.A.), CNRS UMR 6014 & FR3038, Institut de Recherche en Chimie Organique Fine (I.R.C.O.F.) rue Tesnière, 76130 Mont Saint-Aignan, France.

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http://dx.doi.org/10.1016/j.ejmech.2012.11.030DOI Listing
January 2013

Small-molecule inducers of Aβ-42 peptide production share a common mechanism of action.

FASEB J 2012 Dec 12;26(12):5115-23. Epub 2012 Sep 12.

Laboratory of Molecular and Cellular Neuroscience, The Rockefeller University, 1230 York Ave., New York, NY 10021, USA.

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http://dx.doi.org/10.1096/fj.12-212985DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3509055PMC
December 2012

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.

Eur J Med Chem 2012 Dec 16;58:171-83. Epub 2012 Oct 16.

Université de Rouen, Laboratoire de Chimie Organique et Bio-organique, Réactivité et Analyse, CNRS UMR 6014 & FR3038, Institut de Recherche en Chimie Organique Fine rue Tesnière, 76130 Mont Saint-Aignan, France.

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http://linkinghub.elsevier.com/retrieve/pii/S022352341200609
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http://dx.doi.org/10.1016/j.ejmech.2012.10.006DOI Listing
December 2012

Synthesis and biological evaluation of 2,3-diarylimidazo[1,2-a]pyridines as antileishmanial agents.

Eur J Med Chem 2012 Dec 2;58:543-56. Epub 2012 Nov 2.

Université de Nantes, Nantes Atlantique Universités, Laboratoire de Chimie Thérapeutique, Cibles et Médicaments des Infections et du Cancer, IICiMed UPRES EA 1155, UFR des Sciences Pharmaceutiques et Biologiques, 1 rue Gaston Veil, 44035 Nantes, France.

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http://dx.doi.org/10.1016/j.ejmech.2012.10.048DOI Listing
December 2012

Synthesis of N,N'-bis(5-arylidene-4-oxo-3,5-dihydro-4H-imidazol-2-yl)diamines bearing various linkers and biological evaluation as potential inhibitors of kinases.

Eur J Med Chem 2012 Dec 7;58:581-90. Epub 2012 Sep 7.

Université de Rennes 1, Institut des Sciences Chimiques de Rennes, UMR CNRS 6226, groupe Ingénierie Chimique et Molécules pour Vivant, Bât. 10A, Campus de Beaulieu, Avenue du Général Leclerc, CS 74205, 35042 Rennes Cedex, France.

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http://dx.doi.org/10.1016/j.ejmech.2012.08.044DOI Listing
December 2012

Synthesis of New N,N'-Bis(5-arylidene-4-oxo-4,5-dihydrothiazolin-2-yl)piperazine Derivatives Under Microwave Irradiation and Preliminary Biological Evaluation.

Sci Pharm 2012 Oct-Dec;80(4):825-36. Epub 2012 Sep 16.

Université de Rennes 1, Institut des Sciences Chimiques de Rennes (ISCR), UMR CNRS 6226, groupe Ingénièrie Chimique et Molécules pour le Vivant (ICMV), Bât. 10A, campus de Beaulieu, Avenue du Général Leclerc, CS 74205, 35042 Rennes Cedex, France. ; Université d'Abobo-Adjamé, Laboratoire de Chimie Bioorganique et de Subtances Naturelles (LCBSN), BP 802, Abidjan 02, République de la Côte d'Ivoire.

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http://dx.doi.org/10.3797/scipharm.1206-04DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3528043PMC
December 2012

Catalyst-free synthesis of quinazolin-4-ones from (hetero)aryl-guanidines: application to the synthesis of pyrazolo[4,3-f]quinazolin-9-ones, a new family of DYRK1A inhibitors.

Mol Divers 2012 Nov 19;16(4):659-67. Epub 2012 Sep 19.

Département de Pharmacochimie Moléculaire, UMR 5063 & ICMG FR-2607, CNRS/Université Joseph Fourier, BP 53, 38041 Grenoble Cedex 9, France.

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http://dx.doi.org/10.1007/s11030-012-9397-7DOI Listing
November 2012

Synthesis and biological evaluation of new 5-benzylated 4-oxo-3,4-dihydro-5H-pyridazino[4,5-b]indoles as PI3Kα inhibitors.

Eur J Med Chem 2012 Nov 10;57:225-33. Epub 2012 Sep 10.

Université de Nantes, Nantes Atlantique Universités, Laboratoire de Chimie Thérapeutique, Cibles et Médicaments des Infections et du Cancer, IICIMED-EA 1155, UFR Sciences Pharmaceutiques, 1 rue Gaston Veil, Nantes F-44035 Cedex 1, France.

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http://dx.doi.org/10.1016/j.ejmech.2012.09.001DOI Listing
November 2012

Use of ATP analogs to inhibit HIV-1 transcription.

Virology 2012 Oct 6;432(1):219-31. Epub 2012 Jul 6.

National Center for Biodefense and Infectious Diseases, George Mason University, Manassas, VA 20110, USA.

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http://dx.doi.org/10.1016/j.virol.2012.06.007DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3431923PMC
October 2012

Synthesis and biological evaluation of selective and potent cyclin-dependent kinase inhibitors.

Eur J Med Chem 2012 Oct 1;56:210-6. Epub 2012 Sep 1.

ManRos Therapeutics, Centre de Perharidy, Hôtel de recherche, 29680 Roscoff, France.

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http://dx.doi.org/10.1016/j.ejmech.2012.08.033DOI Listing
October 2012

Human cells enter mitosis with damaged DNA after treatment with pharmacological concentrations of genotoxic agents.

Biochem J 2012 Sep;446(3):373-81

Cancer Cell Laboratory, Department of Biological Sciences, 4401 University Drive, University of Lethbridge, Lethbridge, AB, Canada, T1K 3M4.

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http://biochemj.org/lookup/doi/10.1042/BJ20120385
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http://dx.doi.org/10.1042/BJ20120385DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3430003PMC
September 2012

Synthesis and biological evaluation of analogs of the marine alkaloids granulatimide and isogranulatimide.

Eur J Med Chem 2012 Aug 21;54:626-36. Epub 2012 Jun 21.

Laboratoire de Synthèse et Physicochimie de Molécules d'Intérêt Biologique, Université Paul Sabatier, UMR CNRS 5068, 118 route de Narbonne, 31062 Toulouse Cédex 9, France.

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http://dx.doi.org/10.1016/j.ejmech.2012.06.012DOI Listing
August 2012

Library-based discovery of DYRK1A/CLK1 inhibitors from natural product extracts.

Planta Med 2012 Jun 6;78(10):951-6. Epub 2012 Jun 6.

Division of Pharmaceutical Biology, University of Basel, Basel, Switzerland.

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http://dx.doi.org/10.1055/s-0031-1298625DOI Listing
June 2012

[Search for natural substances with therapeutic activity: Pierre Potier (1934-2006)].

Med Sci (Paris) 2012 May 30;28(5):534-42. Epub 2012 May 30.

CNRS, USR3151, phosphorylation de protéines et pathologies humaines, station biologique, 29680 Roscoff, France.

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http://dx.doi.org/10.1051/medsci/2012285020DOI Listing
May 2012

Synthesis of chromeno[3,4-b]indoles as Lamellarin D analogues: a novel DYRK1A inhibitor class.

Eur J Med Chem 2012 Mar 25;49:379-96. Epub 2012 Jan 25.

Institut de Chimie Organique et Analytique, Université d'Orléans, Orléans, France.

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http://dx.doi.org/10.1016/j.ejmech.2012.01.040DOI Listing
March 2012

Synthesis, biological evaluation, and molecular modeling of natural and unnatural flavonoidal alkaloids, inhibitors of kinases.

J Med Chem 2012 Mar 1;55(6):2811-9. Epub 2012 Mar 1.

Centre de Recherche de Gif, Institut de Chimie des Substances Naturelles (ICSN), CNRS, 91198 Gif-sur-Yvette Cedex, France.

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http://dx.doi.org/10.1021/jm201727wDOI Listing
March 2012

[Cell cycle and molecular targets: CDK inhibition].

Bull Cancer 2012 Feb;99(2):163-71

HIA Legouest, service de médecine interne, BP 90001, 57077 Metz Cedex 3, France.

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http://dx.doi.org/10.1684/bdc.2011.1383DOI Listing
February 2012

An efficient approach to dispacamide A and its derivatives.

Org Biomol Chem 2012 Feb 8;10(5):978-87. Epub 2011 Dec 8.

Université de Rennes 1, Laboratoire Sciences Chimiques de Rennes, UMR CNRS 6226, Groupe Ingénierie Chimique & Molécules pour le Vivant (ICMV), Campus de Beaulieu, Rennes, France.

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http://dx.doi.org/10.1039/c1ob06161eDOI Listing
February 2012

A practical approach to new (5Z) 2-alkylthio-5-arylmethylene-1-methyl-1,5-dihydro-4H-imidazol-4-one derivatives.

Molecules 2011 Aug 30;16(9):7377-90. Epub 2011 Aug 30.

Chemical Engineering & Molecules for Life Sciences Group, Université de Rennes 1, Sciences Chimiques de Rennes (SCR), UMR CNRS 6226, Bât. 10A, Campus de Beaulieu, Avenue du Général Leclerc, CS 74205, 35042 Rennes Cedex, France.

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http://dx.doi.org/10.3390/molecules16097377DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6264224PMC
August 2011