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Thierry BESSON

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Straightforward Access to a New Class of Dual DYRK1A/CLK1 Inhibitors Possessing a Simple Dihydroquinoline Core

Mihaela-Liliana Ţînţaş , Ludovic Peauger , Florent Alix , Cyril Papamicaël , Thierry Besson
Molecules, 2023, 28 (1), pp.36. ⟨10.3390/molecules28010036⟩
Journal articles hal-03922046v1

Review on the Synthesis and Therapeutic Potential of Pyrido[2,3-d], [3,2-d], [3,4-d] and [4,3-d]pyrimidine Derivatives

Joana F. Campos , Thierry Besson , Sabine Berteina-Raboin
Pharmaceuticals, 2022, 15 (3), pp.352. ⟨10.3390/ph15030352⟩
Journal articles hal-03890845v1

A skills framework integrating professionally relevant medicinal chemistry proficiencies to strengthen the contemporary practice of pharmacy

C. Decombat , O. Duval , T. Besson , L. Bourel , M. Pudlo
Annales Pharmaceutiques Françaises, 2022, 80 (2), pp.176-186. ⟨10.1016/j.pharma.2021.07.001⟩
Journal articles hal-03581421v1

Copper-Catalyzed C–H Arylation of Fused-Pyrimidinone Derivatives Using Diaryliodonium Salts

Alexandra Pacheco-Benichou , Eugénie Ivendengani , Ioannis Kostakis , Thierry Besson , Corinne Fruit
Catalysts, 2021, 11 (1), pp.28. ⟨10.3390/catal11010028⟩
Journal articles hal-03117643v1

DYRK1A regulates B cell acute lymphoblastic leukemia through phosphorylation of FOXO1 and STAT3

Rahul Bhansali , Malini Rammohan , Paul Lee , Anouchka Laurent , Qiang Wen
Journal of Clinical Investigation, 2021, 131 (1), ⟨10.1172/JCI135937⟩
Journal articles hal-03117656v1

Demonstration of Green Solvent Performance on O,S,N-Heterocycles Synthesis: Metal-Free Click Chemistry and Buchwald—Hartwig Coupling

Joana Campos , Manon Cailler , Remi Claudel , Benjamin Prot , Sabine Berteina-Raboin
Molecules, 2021, 26 (4), pp.1074. ⟨10.3390/molecules26041074⟩
Journal articles hal-03190807v1

Recent Advances in Transition-Metal-Free Late-Stage C-H and N-H Arylation of Heteroarenes Using Diaryliodonium Salts

Thierry Besson , Corinne Fruit
Pharmaceuticals, 2021, 14 (7), pp.661. ⟨10.3390/ph14070661⟩
Journal articles hal-03358321v1

Synthesis of Benzo-Fused 11H-Pyrido[2,1-b]quinazolin-11-ones by a Buchwald–Hartwig Coupling/Pyridine Dearomatization Sequence in Eucalyptol

Joana Campos , Alexandra Pacheco-Benichou , Corinne Fruit , Thierry Besson , Sabine Berteina-Raboin
Synthesis: Journal of Synthetic Organic Chemistry, 2020, ⟨10.1055/s-0040-1707158⟩
Journal articles hal-03001681v1

Diaryliodoniums Salts as Coupling Partners for Transition-Metal Catalyzed C- and N-Arylation of Heteroarenes

Alexandra Pacheco-Benichou , Thierry Besson , Corinne Fruit
Catalysts, 2020, 10 (5), pp.483. ⟨10.3390/catal10050483⟩
Journal articles hal-02557380v1

Exploring Kinase Inhibition Properties of 9H-pyrimido[5,4-b]- and [4,5-b]indol-4-amine Derivatives

Yvonnick Loidreau , Carole Dubouilh-Benard , Marie-Renée Nourrisson , Nadège Loaëc , Laurent Meijer
Pharmaceuticals, 2020, 13 (5), pp.89. ⟨10.3390/ph13050089⟩
Journal articles hal-02612282v1

Microwave-Assisted Synthesis of Potential Bioactive Benzo-, Pyrido- or Pyrazino-thieno[3,2-d]pyrimidin-4-amine Analogs of MPC-6827

Yvonnick Loidreau , Marie-Renée Nourrisson , Corinne Fruit , Cécile Corbière , Pascal Marchand
Pharmaceuticals, 2020, 13 (9), pp.202. ⟨10.3390/ph13090202⟩
Journal articles hal-03001666v1

26th Annual GP2A Medicinal Chemistry Conference & 32nd Journées Franco-Belges de Pharmacochimie

Patrick Dallemagne , Christophe Rochais , Pascal Marchand , Thierry Besson
Pharmaceuticals, 2019, 12 (2), pp.73. ⟨10.3390/ph12020073⟩
Journal articles hal-02330438v1

Harnessing a Novel Dyrk1a-Ablim2-MKL1 Regulatory Module in Megakaryocyte Morphogenesis to Enable Scalable Platelet "Pharming"

Kamaleldin Elagib , Ashton Brock , Goar Mosoyan , Cara Clementelli , Lorrie Delehanty
Blood, 2019, 134 (S1), pp.3250-3250. ⟨10.1182/blood-2019-129049⟩
Journal articles hal-02384958v1

DYRK1A Is Regulated By Oncogenic KMT2A and Required for Survival of KMT2A-Rearranged Acute Lymphoblastic Leukemia

Christian Hurtz , Gerald Wertheim , Rahul Bhansali , Anne Lehman , Grace Jeschke
Blood, 2019, 134 (S1), pp.2742-2742. ⟨10.1182/blood-2019-123475⟩
Journal articles hal-02417476v1
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Biological Characterization of 8-Cyclopropyl-2-(pyridin-3-yl)thiazolo[5,4-f]quinazolin-9(8H)-one, a Promising Inhibitor of DYRK1A

Corinne Fruit , Florence Couly , Rahul Bhansali , Malini Rammohan , Mattias F. Lindberg
Pharmaceuticals, 2019, 12 (4), pp.185. ⟨10.3390/ph12040185⟩
Journal articles hal-02417254v1
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Crystal Structure of 6,7-Dihydro-5a,7a,13,14-tetraaza-pentaphene-5,8-dione

Jean Guillon , Maria de Fatima Pereira-Rosenfeld , Noël Pinaud , Thierry Besson , Valérie Thiéry
X-Ray Structure Analysis Online, 2019, 35 (10), pp.57-59. ⟨10.2116/xraystruct.35.57⟩
Journal articles hal-02330806v1
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Synthesis of 2-Mercapto-(2-Oxoindolin-3-Ylidene)Acetonitriles from 3-(4-Chloro-5H-1,2,3-Dithiazol-5-Ylidene)Indolin-2-ones

Boris Letribot , Régis Delatouche , Hervé Rouillard , Antoine Bonnet , Jean-René Chérouvrier
Molecules, 2018, 23 (6), pp.1390. ⟨10.3390/molecules23061390⟩
Journal articles hal-02197268v1

The Chromosome 21 Kinase DYRK1A and Its Substrate FOXO1 Constitute a Novel Therapeutic Pathway in B-ALL

Rahul Bhansali , Malini Rammohan , Ji Heon Paul Lee , Sebastien Malinge , Yi-Chien Tsai
Blood, 2018, 132 (S1), pp.548-548. ⟨10.1182/blood-2018-99-119854⟩
Journal articles hal-02384966v1
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Development of Kinase Inhibitors via Metal-Catalyzed C–H Arylation of 8-Alkyl-thiazolo[5,4-f]-quinazolin-9-ones Designed by Fragment-Growing Studies

Florence Couly , Marine Harari , Carole Dubouilh-Benard , Laëtitia Bailly , Emilie Petit
Molecules, 2018, 23 (9), pp.2181. ⟨10.3390/molecules23092181⟩
Journal articles hal-02024491v1

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

T.L. Nguyen , Corinne Fruit , Y. Hérault , L. Meijer , Thierry Besson
Expert Opinion on Therapeutic Patents, 2017, 27 (11), pp.1183-1199. ⟨10.1080/13543776.2017.1360285⟩
Journal articles hal-02046302v1

Late-Stage C-H Arylation of Thiazolo[5,4- f ]quinazolin-9(8 H)-one Backbone: Synthesis of an Array of Potential Kinase Inhibitors

Florence Couly , Carole Dubouilh-Benard , Thierry Besson , Corinne Fruit
Synthesis: Journal of Synthetic Organic Chemistry, 2017, 49 (20), pp.4615-4622. ⟨10.1055/s-0036-1588434⟩
Journal articles hal-02046272v1

An Unusual Binding Model of the Methyl 9-Anilinothiazolo[5,4-f] quinazoline-2-carbimidates (EHT 1610 and EHT 5372) Confers High Selectivity for Dual-Specificity Tyrosine Phosphorylation-Regulated Kinases

A. Chaikuad , J. Diharce , M. Schröder , Alicia Foucourt , B. Leblond
Journal of Medicinal Chemistry, 2016, 59 (22), pp.10315-10321. ⟨10.1021/acs.jmedchem.6b01083⟩
Journal articles hal-02046195v1

Efficient Microwave-Assisted Synthesis of Methyl 4- or 5-Nitro­anthranilate

Julien Godeau , Anthony Martinet , Vincent Levacher , Corinne Fruit , Thierry Besson
Synthesis: Journal of Synthetic Organic Chemistry, 2016, 48 (20), pp.3504-3508. ⟨10.1055/s-0035-1562484⟩
Journal articles hal-02046207v1
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Synthesis of bioactive 2-(arylamino)thiazolo[5,4-f]-quinazolin-9-ones via the Hügershoff reaction or Cu- catalyzed intramolecular C-S bond formation

Damien Hédou , Carole Dubouilh-Benard , N. Loaëc , L. Meijer , Corinne Fruit
Molecules, 2016, 21 (6), pp.794. ⟨10.3390/molecules21060794⟩
Journal articles hal-02046212v1
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Synthesis of Thiazolo[5,4-f]quinazolin-9(8H)-ones as Multi-Target Directed Ligands of Ser/Thr Kinases

Damien Hédou , Julien Godeau , N. Loaëc , L. Meijer , Corinne Fruit
Molecules, 2016, 21 (5), pp.578. ⟨10.3390/molecules21050578⟩
Journal articles hal-02046213v1

Recent Developments in Microwave-Assisted Metal-Catalyzed C-H Functionalization of Heteroarenes for Medicinal Chemistry and Material Applications

Thierry Besson , Corinne Fruit
Synthesis: Journal of Synthetic Organic Chemistry, 2016, 48 (22), pp.3879-3889. ⟨10.1055/s-0035-1562608⟩
Journal articles hal-02046186v1

Pd-Catalyzed and Copper Assisted Regioselective Sequential C2 and C7 Arylation of Thiazolo[5,4-f]quinazolin-9(8H)-one with Aryl Halides

Marine Harari , Florence Couly , Corinne Fruit , Thierry Besson
Organic Letters, 2016, 18 (13), pp.3282-3285. ⟨10.1021/acs.orglett.6b01552⟩
Journal articles hal-02046211v1

A novel DYRK1A (Dual specificity tyrosine phosphorylation‐regulated kinase 1A) inhibitor for the treatment of Alzheimer's disease: effect on Tau and amyloid pathologies in vitro

S. Coutadeur , H. Benyamine , L. Delalonde , C. de Oliveira , B. Leblond
Journal of Neurochemistry, 2015, 133 (3), pp.440-451. ⟨10.1111/jnc.13018⟩
Journal articles hal-02046148v1

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

Yvonnick Loidreau , Emmanuel Deau , Pascal Marchand , Marie-Renée Nourrisson , Cédric Logé
European Journal of Medicinal Chemistry, 2015, 92, pp.124-134. ⟨10.1016/j.ejmech.2014.12.038⟩
Journal articles hal-01135195v1

Synthesis of polyfunctionalized benzo[d]thiazoles as novel anthranilic acid derivatives

Damien Hédou , Marine Harari , Julien Godeau , Carole Dubouilh-Benard , Corinne Fruit
Tetrahedron Letters, 2015, 56 (27), pp.4088-4092. ⟨10.1016/j.tetlet.2015.05.018⟩
Journal articles hal-01160622v1

Cu/Pd-catalyzed C-2-H arylation of quinazolin-4(3H)-ones with (hetero)aryl halides

Julien Godeau , Marine Harari , Sylvain Laclef , Emmanuel Deau , Corinne Fruit
European Journal of Organic Chemistry, 2015, 2015 (35), pp.7705-7717. ⟨10.1002/ejoc.201501129⟩
Journal articles hal-02046152v1

Ligand-Free Pd-Catalyzed and Copper-Assisted C−H Arylation ofQuinazolin-4-ones with Aryl Iodides under Microwave Heating

Sylvain Laclef , Marine Harari , Julien Godeau , Isabelle Schmitz-Afonso , Laurent Bischoff
Organic Letters, 2015, organic letters, 17 (7), pp.1700-1713. ⟨10.1021/acs.orglett.5b00467⟩
Journal articles hal-01141150v1
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DYRK1A controls the transition from proliferation to quiescence during lymphoid development by destabilizing Cyclin D3

B. J. Thompson , R. Bhansali , L. Diebold , D. E. Cook , L. Stolzenburg
Journal of Experimental Medicine, 2015, 212 (6), pp.723-740. ⟨10.1084/jem.20150002⟩
Journal articles hal-01160621v1

Rational multistep synthesis of a novel polyfunctionalized benzo[d]thiazole and its thiazolo[5,4-b]pyridine analogue

Damien Hédou , Emmanuel Deau , Marine Harari , Morgane Sanselme , Corinne Fruit
Tetrahedron, 2014, 70 (5541-5549), pp.5541-5549. ⟨10.1016/j.tet.2014.06.103⟩
Journal articles hal-01141181v1
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Design and Synthesis of Thiazolo[5,4-f]quinazolines as DYRK1A Inhibitors, Part I

Alicia Foucourt , Damien Hédou , Carole Dubouilh-Benard , Laurent Désiré , Anne-Sophie Casagrande
Molecules, 2014, 19 (10), pp.15546-15571. ⟨10.3390/molecules191015546⟩
Journal articles hal-01141172v1
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Design and Synthesis of Thiazolo[5,4-f]quinazolines as DYRK1A Inhibitors, Part II

Alicia Foucourt , Damien Hédou , Carole Dubouilh-Benard , Angelique Girard , Thierry Taverne
Molecules, 2014, 19 (10), pp.15411-15439. ⟨10.3390/molecules191015411⟩
Journal articles hal-01135223v1

Microwave-assisted synthesis of novel N-(4-phenylthiazol-2-yl)-benzo[d]thiazole-, thiazolo[4,5-b]pyridine-, thiazolo[5,4-b]pyridine- and benzo[d]oxazole-2-carboximidamides inspired by marine topsentines and nortopsentines

Emmanuel Deau , Carole Dubouilh-Benard , Vincent Levacher , Thierry Besson
Tetrahedron, 2014, 70 (35), pp.5532-5540. ⟨10.1016/j.tet.2014.06.102⟩
Journal articles hal-01141178v1

Efficient new synthesis of N-arylbenzo[b]furo[3,2-d]pyrimidin-4-amines and their benzo[b]thieno[3,2-d]pyrimidin-4-amine analogues via a microwave-assisted Dimroth rearrangement

Yvonnick Loidreau , Carole Dubouilh-Benard , Pascal Marchand , Marie-Renée Nourrisson , Muriel Duflos
Journal of Heterocyclic Chemistry, 2013, 50 (5), pp.1187-1197. ⟨10.1002/jhet.1716⟩
Journal articles hal-01015485v1

Discovery of a Novel Broad-Spectrum Antifungal Agent Derived from Albaconazole

Rémi Guillon , Fabrice Pagniez , Carine Picot , Damien Hédou , Alain Tonnerre
ACS Medicinal Chemistry Letters, 2013, 4 (2), pp.288-292. ⟨10.1021/ml300429p⟩
Journal articles hal-01015468v1

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.

Emmanuel Deau , Yvonnick Loidreau , Pascal Marchand , Marie-Renée Nourrisson , Nadège Loaëc
Bioorganic and Medicinal Chemistry Letters, 2013, 23 (24), pp.6784-6788. ⟨10.1016/j.bmcl.2013.10.019⟩
Journal articles hal-00997420v1

Developments in Meyers' lactamization methodology: en route to bi(hetero)aryl structures with defined axial chirality.

Svetlana Postikova , Mohamad Sabbah , Daniel Wightman , Ich Tuan Nguyen , Morgane Sanselme
Journal of Organic Chemistry, 2013, 78 (16), pp.8191-8197. ⟨10.1021/jo401259w⟩
Journal articles hal-00997427v1

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.

Yvonnick Loidreau , Pascal Marchand , Carole Dubouilh-Benard , Marie-Renée Nourrisson , Muriel Duflos
European Journal of Medicinal Chemistry, 2013, 59, pp.283-295. ⟨10.1016/j.ejmech.2012.11.030⟩
Journal articles hal-00997416v1

Suzuki cross-coupling of 5-bromothieno[2,3-b]pyridines for the convenient synthesis of 8-arylpyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-amines

Yvonnick Loidreau , Vincent Levacher , Thierry Besson
Tetrahedron Letters, 2013, 54 (9), pp.1160-1163. ⟨10.1016/j.tetlet.2012.12.077⟩
Journal articles hal-01015472v1

Convenient one-pot synthesis of N3-substituted pyrido[2,3-d]-, pyrido[3,4-d]-, pyrido[4,3-d]-pyrimidin-4(3H)-ones, and quinazolin-4(3H)-ones analogs

Emmanuel Deau , Damien Hédou , Elizabeth Chosson , Vincent Levacher , Thierry Besson
Tetrahedron Letters, 2013, 54 (27), pp.3518-3521. ⟨10.1016/j.tetlet.2013.04.096⟩
Journal articles hal-01015451v1

Novel synthesis of angular thiazolo[5,4-f] and [4,5-h]quinazolines, preparation of their linear thiazolo[4,5-g] and [5,4-g]quinazoline analogs

Damien Hédou , Rémi Guillon , Charlotte Lecointe , Cédric Logé , Elizabeth Chosson
Tetrahedron, 2013, 69 (15), pp.3182-3191. ⟨10.1016/j.tet.2013.02.066⟩
Journal articles hal-01015586v1

Microwave-Assisted [3+2] Cycloaddition and Suzuki-Miyaura Cross-Coupling for a Concise Access to Polyaromatic Scaffolds

Damien Hédou , Emmanuel Deau , Carole Dubouilh-Benard , Morgane Sanselme , Anthony Martinet
European Journal of Organic Chemistry, 2013, 2013 (33), pp.7533-7545. ⟨10.1002/ejoc.201301014⟩
Journal articles hal-01015445v1

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

Yvonnick Loidreau , Pascal Marchand , Carole Dubouilh-Benard , Marie-Renée Nourrisson , Muriel Duflos
European Journal of Medicinal Chemistry, 2012, 58, pp.171-183. ⟨10.1016/j.ejmech.2012.10.006⟩
Journal articles hal-02357785v1

First synthesis of 4-aminopyrido[2′,3′:4,5]furo[3,2-d]pyrimidines

Yvonnick Loidreau , Pascal Marchand , Carole Dubouilh-Benard , Marie-Renée Nourrisson , Muriel Duflos
Tetrahedron Letters, 2012, 53 (8), pp.944-947. ⟨10.1016/j.tetlet.2011.12.042⟩
Journal articles hal-01016753v1

Study of N1-alkylation of indoles from the reaction of 2(or 3)-aminoindole-3-(or 2)carbonitriles with DMF-dialkylacetals

Yvonnick Loidreau , Sigismund Melissen , Vincent Levacher , Cédric Logé , Jérôme Graton
Organic & Biomolecular Chemistry, 2012, 10 (25), pp.4916-4925. ⟨10.1039/c2ob25747e⟩
Journal articles hal-00997070v1

Synthesis of novel 7-oxo and 7-hydroxy trifluoroallocolchicinoids with cytotoxic effect

Elizabeth Chosson , Francesca Santoro , Christophe Rochais , Jana Sopkova-de Oliveira Santos , Rémi Legay
Bioorganic and Medicinal Chemistry Letters, 2012, 20 (8), pp.2614-2623. ⟨10.1016/j.bmc.2012.02.043⟩
Journal articles hal-02357753v1

Microwave-assisted thermal decomposition of formamide: a tool for coupling a pyrimidine ring with an aromatic partner

Yvonnick Loidreau , Thierry Besson
Tetrahedron, 2011, 67 (26), pp.4852-4857. ⟨10.1016/j.tet.2011.05.010⟩
Journal articles hal-01018135v1
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Structure of Pb2+/dCMP and Pb2+/CMP complexes as characterized by tandem mass spectrometry and IRMPD spectroscopy

Jean-Yves Salpin , Létitia Gamiette , Jeanine Tortajada , Thierry Besson , Philippe Maître
International Journal of Mass Spectrometry, 2011, 304 (2-3), pp.154-164. ⟨10.1016/j.ijms.2010.07.011⟩
Journal articles hal-00619188v1

Binaphthyl platform as starting materials for the preparation of electron rich benzo[g,h,i]perylenes. Application to molecular architectures based on amino benzo[g,h,i]perylenes and carborane combinations.

Grégory Pieters , Anne Gaucher , Damien Prim , Thierry Besson , José Giner Planas
Chemical Communications, 2011, 47 (27), pp.7725-7727. ⟨10.1039/c1cc12099a⟩
Journal articles hal-01018301v1

Microwave-accelerated Dimroth rearrangement for the synthesis of 4-anilino-6-nitroquinazolines. Application to an efficient synthesis of a microtubule destabilizing agent.

Alicia Foucourt , Carole Dubouilh-Benard , Elizabeth Chosson , Cecile Corbiere , Catherine Buquet
Tetrahedron, 2010, 66 (25), pp.4495-4502. ⟨10.1016/j.tet.2010.04.066⟩
Journal articles hal-01020796v1

Erymildbraedin A and B, two novel cytotoxic dimethylpyrano-isoflavones from the stem bark of Erythrina mildbraedii: evaluation of their activity toward endocrine cancer cells.

Ruben F Tchokouaha , Xanthippi Alexi , Elizabeth Chosson , Thierry Besson , Alexios-Leandros Skaltsounis
Journal of Enzyme Inhibition and Medicinal Chemistry, 2010, 25 (2), pp.228-233. ⟨10.3109/14756360903169972⟩
Journal articles hal-01020552v1

First synthesis of 2-aminosubstituted-2-perfluoroalkyl-3,6-dihydro-2H-thiopyrans by hetero-Diels-Alder reactions of fluorinated thioamides under microwave heating

Sergey S Mikhailichenko , J.-P. Bouillon , Thierry Besson , Yuryi G Shermolovich
Tetrahedron Letters, 2010, 51 (6), pp.990-993. ⟨10.1016/j.tetlet.2009.12.064⟩
Journal articles hal-01019603v1

Synthesis and antitumoral activity of novel thiazolobenzotriazole, thiazoloindolo[3,2-c]quinoline and quinolinoquinoline derivatives

Anne Beauchard , Alexis Jaunet , Laurence Murillo , Brigitte Baldeyrou , Amélie Lansiaux
European Journal of Medicinal Chemistry, 2009, 44 (10), pp.3858-3865. ⟨10.1016/j.ejmech.2009.04.012⟩
Journal articles hal-01449310v1

Synthesis and kinase inhibitory activity of novel substituted indigoids.

Anne Beauchard , Hélène Laborie , Hervé Rouillard , Olivier Lozach , Yoan Ferandin
Bioorganic and Medicinal Chemistry, 2009, 17 (17), pp.6257-63. ⟨10.1016/j.bmc.2009.07.051⟩
Journal articles hal-00416031v1

Synthesis and kinase inhibitory activity of novel substituted indigoids

Anne Beauchard , Helene Laborie , Hervé Rouillard , Olivier Lozach , Yoan Ferandin
Bioorganic and Medicinal Chemistry Letters, 2009, 17 (17), pp.6257-6263. ⟨10.1016/j.bmc.2009.07.051⟩
Journal articles hal-02357759v1

Microwave-assisted synthesis of alpha-ethoxycarbamates

Alexandre Lumbroso , Floris Chevallier , Isabelle Beaudet , Jean-Paul Quintard , Thierry Besson
Tetrahedron, 2009, 65 (45), pp.9180-9187. ⟨10.1016/j.tet.2009.09.023⟩
Journal articles hal-02143508v1

Structure of electron-capture dissociation fragments from charge-tagged peptides probed by tunable infrared multiple photon dissociation.

Gilles Frison , Guillaume van Der Rest , Frantisek Turecek , Thierry Besson , Joël Lemaire
Journal of the American Chemical Society, 2008, 130 (45), pp.14916-14917. ⟨10.1021/ja805257v⟩
Journal articles hal-00467063v1

Synthesis and evaluation of the antimicrobial activity of novel quinazolinones

Maria de Fatima Pereira , Romain Chevrot , Eric Rosenfeld , Valérie Thiéry , Thierry Besson
Journal of Enzyme Inhibition and Medicinal Chemistry, 2008, 22 (5), pp.577-583. ⟨10.1080/14756360701425345⟩
Journal articles hal-01960717v1

Novel 9-oxo-thiazolo[5,4-f]quinazoline-2-carbonitrile derivatives as dual cyclin-dependent kinase 1 (CDK1)/glycogen synthase kinase-3 (GSK-3) inhibitors: Synthesis, biological evaluation and molecular modeling studies

Cédric Logé , Alexandra Testard , Valérie Thiéry , Olivier Lozach , Mélina Blairvacq
European Journal of Medicinal Chemistry, 2008, 43 (7), pp.1469-1477. ⟨10.1016/j.ejmech.2007.09.020⟩
Journal articles hal-02357774v1

Microwave-assisted Synthesis of Novel Thiazolocarbazoles and Evaluation as Potential Anticancer Agents. Part III

Alexandra Testard , Laurent Picot , Ingrid Fruitier-Arnaudin , Jean-Marie Piot , Hadjila Chabane
Journal of Enzyme Inhibition and Medicinal Chemistry, 2008, 19 (6), pp.467-473. ⟨10.1080/14756360412331280491⟩
Journal articles hal-01967795v1
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Tautomerism of uracil probed via IR spectroscopy of singly hydrated uracil.

Joost M. Bakker , Thierry Besson , Maurizio Brugnara , Paolo Tosi , Jean-Yves Salpin
Journal of Physical Chemistry A, 2008, 112 (48), pp.12393-12400. ⟨10.1021/jp806396t⟩
Journal articles hal-00368127v1

Synthesis of latonduine derivatives via intramolecular Heck coupling reaction

A. Putey , L. Joucla , L. Picot , Thierry Besson , B. Joseph.
Tetrahedron, 2007, pp.63, 867
Journal articles hal-00158714v1

Synthesis and antiproliferative activity of clausine E, mukonine, and koenoline bioisosteres

François Liger , Florence Popowycz , Thierry Besson , Laurent Picot , Carlos Galmarini
Bioorganic and Medicinal Chemistry Letters, 2007, 15 (16), pp.5615-5619. ⟨10.1016/j.bmc.2007.05.033⟩
Journal articles hal-02357763v1

On the origin of some cubebene derivatives — Diels–Alder adducts and the diene structures of solidago compounds

Christopher Jankowski , André Pelletier , Eduardo Diaz T. , Jacqueline M.R Belanger , Jocelyn J.R Paré
Canadian Journal of Chemistry, 2007, 85 (11), pp.996-1005. ⟨10.1139/V07-112⟩
Journal articles hal-02357729v1

Synthesis of novel 2,3-condensed thieno[2,3- d ]pyrimidin-4-ones via Appel's salt chemistry

Maria de Fatima Pereira , Valérie Thiéry , Thierry Besson
Journal of Sulfur Chemistry, 2006, 27 (1), pp.49-55. ⟨10.1080/17415990500493213⟩
Journal articles hal-02357738v1

Synthesis of novel 5-substituted indirubins as protein kinases inhibitors

Anne Beauchard , Yoan Ferandin , Stéphane Frère , Olivier Lozach , Mélina Blairvacq
Bioorganic and Medicinal Chemistry, 2006, 14 (18), pp.6434-43. ⟨10.1016/j.bmc.2006.05.036⟩
Journal articles hal-00169371v1

Thiazolo[5,4-f]quinazolin-9-ones, inhibitors of glycogen synthase kinase-3

Alexandra Testard , Cédric Logé , Benoît Léger , Jean-Michel Robert , Olivier Lozach
Bioorganic and Medicinal Chemistry Letters, 2006, 16 (13), pp.3419-3423. ⟨10.1016/j.bmcl.2006.04.006⟩
Journal articles hal-02357746v1

Synthesis and evaluation of the antiproliferative activity of novel thiazoloquinazolinone kinases inhibitors.

Alexandra Testard , Laurent Picot , Olivier Lozach , Melina Blairvacq , Laurent Meijer
Journal of Enzyme Inhibition and Medicinal Chemistry, 2005, 20 (6), pp.557-568. ⟨10.1080/14756360500212399⟩
Journal articles hal-01443570v1

Eco-Friendly Microwave-Assisted Scaleable Synthesis of 2-Cyanobenzothiazoles via N -Arylimino-1,2,3-dithiazoles

Stéphane Frère , Valérie Thiéry , Thierry Besson
Synthetic Communications, 2003, 33 (21), pp.3795-3804. ⟨10.1081/SCC-120025190⟩
Journal articles hal-02357713v1

Eco-Friendly Microwave-Assisted Scaleable Synthesis of 2-Cyanobenzothiazoles via N -Arylimino-1,2,3-dithiazoles

Valérie Thiéry , Thierry Besson
Synthetic Communications, 2003, 33 (21), pp.3795-3804. ⟨10.1081/SCC-120025190⟩
Journal articles hal-02357727v1

Efficient solvent-free microwave phosphorylation of microcrystalline cellulose

Natalia Gospodinova , Axelle Grelard , Marc Jeannin , Gabrielle Chitanu , Adrian Carpov
Green Chemistry, 2002, 4 (3), pp.220-222. ⟨10.1039/b200295g⟩
Journal articles hal-02357733v1

Rapid synthesis of 2-cyanobenzothiazole, isothiocyanate and cyanoformanilide derivatives of dapsone †

Thierry Besson , Jérôme Guillard , Charles Rees
Journal of the Chemical Society, Perkin Transactions 1, 2000, 4, pp.563-566. ⟨10.1039/a908742g⟩
Journal articles hal-02357789v1

Imidazoquinolinethiones from 8-aminoquinolines by a novel peri-participation

Thierry Besson , Charles Rees , David Roe , Valérie Thiéry
Journal of the Chemical Society, Perkin Transactions 1, 2000, 4, pp.555-561. ⟨10.1039/a908952g⟩
Journal articles hal-02357793v1

Fe and H2O2 distributions in the upper water column in the Indian sector of the Southern Ocean

Géraldine Sarthou , C. Jeandel , Laurence Brisset , David Amouroux , Thierry Besson
Earth and Planetary Science Letters, 1998, 147 (1-4), pp.83-92. ⟨10.1016/S0012-821X(97)00004-6⟩
Journal articles hal-00456475v1

N-(Cyanothioformyl)indoline; a new indoline ring forming reaction

Thierry Besson , Gerald Guillaumet , Christelle Lamazzi , Charles Rees , Valérie Thiéry
Journal of the Chemical Society, Perkin Transactions 1, 1998
Journal articles hal-02357800v1

Rapid Synthesis of 2-Cyanobenzothiazoles from N -Aryliminodithiazoles Under Microwave Irradiation

Valérie Bénéteau , Thierry Besson , Charles Rees
Synthetic Communications, 1997, 27 (13), pp.2275-2280. ⟨10.1080/00397919708003382⟩
Journal articles hal-02357709v1

Synthesis of a benzodioxinic analog of 8-methoxypsoralen

Thierry Besson , Nicolas Ruiz , Gérard Coudert , Gerald Guillaumet
Tetrahedron, 1995, 51 (11), pp.3197-3204. ⟨10.1016/0040-4020(95)00058-G⟩
Journal articles hal-02889857v1

3,1-Benzoxazin-4-ones, 3,1-benzothiazin-4-ones and N-arylcyanothioformamides

Thierry Besson , Kumaraswamy Emayan , Charles Rees
Journal of the Chemical Society, Chemical Communications, 1995, 14, pp.1419. ⟨10.1039/C39950001419⟩
Journal articles hal-02357768v1

Biophysical and biological properties of newly synthesized dioxinocoumarin derivatives

Gabriella Csík , Györgyi Rontó , Silvano Nocentini , Simone Averbeck , Dietrich Averbeck
Journal of Photochemistry and Photobiology B: Biology, 1994, 24 (2), pp.129-139. ⟨10.1016/1011-1344(94)07015-6⟩
Journal articles hal-02889856v1

Convenient synthesis of 5-substituted-6-methoxy or 6-hydroxy-2,3-dihydro-1,4-benzodioxins via lithiated intermediates

Thierry Besson , Mohamed Hretani , Gérard Coudert , Gerald Guillaumet
Tetrahedron, 1993, 49 (7), pp.1421-1430. ⟨10.1016/S0040-4020(01)90194-2⟩
Journal articles hal-02889858v1

Mitsunobu Thiofunctionalization-Part 2. 1 an Expedient Synthesis of Aza-Heterocycle/Thiosugar Hybrids

Thierry Besson , Mamdouh Al Neirabeyeh , Marie-Claude Viaud , Patrick Rollin
Synthetic Communications, 1990, 20 (11), pp.1631-1639. ⟨10.1080/00397919008053083⟩
Journal articles hal-02357706v1

A mild One-Step Procedure for the Synthesis of β-Iodo Epoxides from the Corresponding Epoxy-Alcohols

Thierry Besson , Patrick Rollin
Synthetic Communications, 1990, 20 (19), pp.3039-3044. ⟨10.1080/00397919008051523⟩
Journal articles hal-02357707v1

Conception et synthèses d'inhibiteurs de la kinase DYRK1A

Thierry Besson
Séminaire national, Faculté de pharmacie de l'Université de Tours, Jun 2018, Tours, France
Conference papers hal-02391097v1

Conception of DYRK1A kinase inhibitors via metal-catalyzed C-H arylation, inspired by fragment-growing studies

Florence Couly , Julien Diharce , Pascal Bonnet , Meijer Laurent , Corinne Fruit
International Electronic Conference on Medicinal Chemistry (ECMC, 4, 2018), Jean-Jacques Vanden Eynde (coord.), Nov 2018, [online], Belgium. ⟨10.3390/ecmc-4-05580⟩
Conference papers hal-02383907v1

Promising DYRK1A inhibitor synthesized by late-stage C-H Arylation

Florence Couly , Corinne Fruit , Thierry Besson
Journées franco-belges de chimie thérapeutique (JFB, 32, 2018) - Conférences européennes des pharmacochimistes de l'Arc Atlantique (GP2A, 26, 2018), Jun 2018, Asnelles-sur-Mer, France
Conference papers hal-02384759v1

Design and synthesis of DYRK's family kinases inhibitors against neurodegenerative diseases

Thierry Besson
Séminaire international, Katholieke Universiteit Leuven (KU), Jun 2017, Louvain, Belgium
Conference papers hal-02390455v1

Design and synthesis of DYRK's family kinases inhibitors against neurodegenerative diseases

Thierry Besson
Séminaire international, Universiteit Gent, Jun 2017, Gand, Belgium
Conference papers hal-02390460v1

Late-stage C-H Arylation of Thiazolo[5,4-f]quinazolin-9(8H)-one Backbone: Synthesis of an Array of Potential Kinase Inhibitors

Florence Couly , Carole Dubouilh-Benard , Meijer Laurent , Corinne Fruit , Thierry Besson
International Electronic Conference on Medicinal Chemistry (ECMC, 3, 2017), Jean-Jacques Vanden Eynde, Nov 2017, [online], Belgium. ⟨10.3390/ecmc-3-04650⟩
Conference papers hal-02383887v1

Synthesis of Bioactive 2-(arylamino)thiazolo[5,4-f]-quinazolin-9-ones via the Hügershoff Reaction or Cu- Catalyzed Intramolecular C-S Bond Formation

Damien Hédou , Carole Dubouilh-Benard , Nadège Loaëc , Meijer Laurent , Corinne Fruit
International Electronic Conference on Medicinal Chemistry (ECMC, 2, 2016), Jean-Jacques Vanden Eynde (coord.), Nov 2016, [online], Belgium. ⟨10.3390/ecmc-2-A010⟩
Conference papers hal-02383867v1

Thiazolo[5,4-f]quinazolines as DYRK Kinases inhibitors

Thierry Besson
Journées franco-belges de pharmacochimie (JFB, 30, 2016), May 2016, Amboise, France
Conference papers hal-02379426v1

Late-Stage Sequential C-H Functionalization of Thiazolo[5,4-f]quina-zolin-9(8H)-one: Synthesis of a Library of Potential Kinase Inhibitors

Corinne Fruit , Florence Couly , Marine Harari , Vincent Levacher , Thierry Besson
International Electronic Conference on Synthetic Organic Chemistry (ECSOC, 20, 2016), Julio A. Seijas Vázquez (coord.), Nov 2016, [online], Spain
Conference papers hal-02383920v1

Kinase inhibitors and microwave-assisted chemistry, a nice story

Thierry Besson
Séminaire national, Université de Versailles Saint-Quentin (UVSQ), Sep 2015, Amiens, France
Conference papers hal-02390779v1

Microwave-assisted C-H arylation of Quinazolin-4-one-type Precursors of Bioactive Heterocycles

Corinne Fruit , Julien Godeau , Marine Harari , Vincent Levacher , Thierry Besson
International Electronic Conference on Medicinal Chemistry (ECMC, 1, 2015), Jean-Jacques Vanden Eynde (coord.), Nov 2015, [online], Belgium. ⟨10.3390/ecmc-1-A004⟩
Conference papers hal-02383839v1

Kinase inhibitors and microwave-assisted chemistry, a nice story

Thierry Besson
Séminaire national, Université de Picardie Jules Verne (UPJV), Jun 2015, Amiens, France
Conference papers hal-02390509v1

Ligand-free Pd/Cu-catalyzed microwave-assisted C-H arylation of quinazolin-4(3H)-ones with aryl iodides

Marine Harari , Corinne Fruit , Thierry Besson
Semaine d'études en chimie organique (SECO, 52, 2015), May 2015, Morzine, France
Conference papers hal-02378695v1

Microwave extraction of bioactive molecules

E. Destandau , S. Zubrzycki , C. Elfakir , Abdelhakim Elomri , Thierry Besson
Cosmetic innovation days (COSMINNOV, 2013), Oct 2013, Orléans, France
Conference papers hal-02550339v1

IRMPD spectroscopy and quantum chemistry: two ideal partners for probing the structure of gaseous ions

Jean-Yves Salpin , Edith Nicol , Thierry Besson , William Buchmann , Marie-Pierre Gaigeot
35th congress of theoretical chemists of latin expression 35th QUITEL, Sep 2009, San Andres, Colombia
Conference papers hal-00514248v1

Interaction of Pb2+ ions with nucleic acids building blocks: tandem mass spectrometry and IRMPD spectroscopy

Jean-Yves Salpin , Jeanine Tortajada , Thierry Besson , Joel Lemaire , Debora Scuderi
Isolated Biomolecules and Biomolecular interactions, Apr 2008, Valladolid, Spain
Conference papers hal-00275019v1