Thierry BESSON

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DYRK1A inhibition results in MYC and ERK activation rendering KMT2A-R acute lymphoblastic leukemia cells sensitive to BCL2 inhibition

V S S Abhinav Ayyadevara , Gerald Wertheim , Shikha Gaur , John A Chukinas , Joseph P Loftus et al.

Leukemia, 2025, 39 (5), pp.1078-1089. ⟨10.1038/s41375-025-02575-w⟩

Article dans une revue hal-05175869v1
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Quinazoline-Derivatives of Imino-1,2,3-Dithiazoles Promote Biofilm Dispersion of Pseudomonas aeruginosa

Mathieu Gonzalez , Anne-Sophie Tareau , Daphnée de Crozals , Corentin Layec , Nathan Broudic et al.

Pharmaceuticals, 2025, 18 (11), pp.1733. ⟨10.3390/ph18111733⟩

Article dans une revue hal-05469128v1

Synthesis of Thiazole-fused Tricyclic Quinazolinone Alkaloids and Their Derivatives

Nathan Broudic , Corentin Layec , Corinne Fruit , Thierry Besson

Synthesis: Journal of Synthetic Organic Chemistry, 2024, 56 (09), pp.1485-1497. ⟨10.1055/a-2243-4727⟩

Article dans une revue hal-05175907v1
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Novel Thiazole-Fused [4,5-g] or [5,4-g]Quinazolin-8-ones and Their Quinazoline Analogues: Synthesis and Biological Evaluation

Nathan Broudic , Alexandra Pacheco-Benichou , Cecile Corbiere , Blandine Baratte , Thomas Robert et al.

Pharmaceuticals, 2024, 17 (11), pp.1452. ⟨10.3390/ph17111452⟩

Article dans une revue hal-04783236v1
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Contribution of Professor Charles Rees to the development of the chemistry of disulfur dichloride

Thierry Besson , Lidia S Konstntinova , Panayiotis A Koutentis , Oleg A Rakitin , Sivaprasad Sivadasan et al.

ARKIVOC - Online Journal of Organic Chemistry, 2024, Commemorative Issue in Honor of Prof. Alan R. Katritzky and Prof. Charles Rees on the occasion of the 25th anniversary of the first publication of Arkivoc (Archive for Organic Chemistry), 2024 (1), ⟨10.24820/ark.5550190.p012.136⟩

Article dans une revue hal-04432826v1

Efficacy of DYRK1A inhibitors in novel models of Down syndrome acute lymphoblastic leukemia

Shannon Carey-Smith , Maryam Simad , Kunjal Panchal , Carlos Aya-Bonilla , Hannah Smolders et al.

Haematologica, 2024, ⟨10.3324/haematol.2023.284271⟩

Article dans une revue hal-04493069v1
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Synthesis of Trifunctional Thiazole-Fused Anthranilonitrile and Anthranilic Acid Derivatives

Nathan Broudic , Alexandra Pacheco-Benichou , Corinne Fruit , Thierry Besson

Synthesis: Journal of Synthetic Organic Chemistry, 2023, 55 (20), pp.3263-3271. ⟨10.1055/a-2086-3015⟩

Article dans une revue hal-04421061v1
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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 et al.

Molecules, 2023, 28 (1), pp.36. ⟨10.3390/molecules28010036⟩

Article dans une revue hal-03922046v1

Photocatalyst-Free, Visible-Light-Mediated C–H Perfluoroalkylation of Quinazolin-4(3H)-ones with perfluoroalkyl Iodides

Thomas Delouche , Abdoul Gadiry-Diallo , Thierry Besson , Sensuke Ogoshi , Corinne Fruit

Synthesis: Journal of Synthetic Organic Chemistry, 2023, 55 (21), pp.3670-3684. ⟨10.1055/a-2054-0482⟩

Article dans une revue hal-04421057v1
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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⟩

Article dans une revue hal-03581421v1
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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⟩

Article dans une revue hal-03890845v1

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

Rahul Bhansali , Malini Rammohan , Paul Lee , Anouchka Laurent , Qiang Wen et al.

Journal of Clinical Investigation, 2021, 131 (1), ⟨10.1172/JCI135937⟩

Article dans une revue hal-03117656v1
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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⟩

Article dans une revue hal-03358321v1
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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 et al.

Molecules, 2021, 26 (4), pp.1074. ⟨10.3390/molecules26041074⟩

Article dans une revue hal-03190807v1
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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⟩

Article dans une revue hal-03117643v1
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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 et al.

Pharmaceuticals, 2020, 13 (9), pp.202. ⟨10.3390/ph13090202⟩

Article dans une revue hal-03001666v1

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⟩

Article dans une revue hal-03001681v1
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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 et al.

Pharmaceuticals, 2020, 13 (5), pp.89. ⟨10.3390/ph13050089⟩

Article dans une revue hal-02612282v2

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⟩

Article dans une revue hal-02557380v1

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 et al.

Blood, 2019, 134 (S1), pp.2742-2742. ⟨10.1182/blood-2019-123475⟩

Article dans une revue 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 et al.

Pharmaceuticals, 2019, 12 (4), pp.185. ⟨10.3390/ph12040185⟩

Article dans une revue 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 et al.

X-Ray Structure Analysis Online, 2019, 35 (10), pp.57-59. ⟨10.2116/xraystruct.35.57⟩

Article dans une revue hal-02330806v1

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 et al.

Blood, 2019, 134 (S1), pp.3250-3250. ⟨10.1182/blood-2019-129049⟩

Article dans une revue hal-02384958v1
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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⟩

Article dans une revue hal-02330438v1
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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 et al.

Molecules, 2018, 23 (6), pp.1390. ⟨10.3390/molecules23061390⟩

Article dans une revue 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 et al.

Blood, 2018, 132 (S1), pp.548-548. ⟨10.1182/blood-2018-99-119854⟩

Article dans une revue 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 et al.

Molecules, 2018, 23 (9), pp.2181. ⟨10.3390/molecules23092181⟩

Article dans une revue 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⟩

Article dans une revue 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⟩

Article dans une revue hal-02046272v1

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⟩

Article dans une revue hal-02046207v1

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⟩

Article dans une revue hal-02046186v1
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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 et al.

Molecules, 2016, 21 (5), pp.578. ⟨10.3390/molecules21050578⟩

Article dans une revue hal-02046213v1
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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 et al.

Molecules, 2016, 21 (6), pp.794. ⟨10.3390/molecules21060794⟩

Article dans une revue hal-02046212v1

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 et al.

Journal of Medicinal Chemistry, 2016, 59 (22), pp.10315-10321. ⟨10.1021/acs.jmedchem.6b01083⟩

Article dans une revue hal-02046195v1

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⟩

Article dans une revue hal-02046211v1

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 et al.

European Journal of Medicinal Chemistry, 2015, 92, pp.124-134. ⟨10.1016/j.ejmech.2014.12.038⟩

Article dans une revue hal-01135195v1

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 et al.

Journal of Neurochemistry, 2015, 133 (3), pp.440-451. ⟨10.1111/jnc.13018⟩

Article dans une revue hal-02046148v1

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

Damien Hédou , Marine Harari , Julien Godeau , Carole Dubouilh-Benard , Corinne Fruit et al.

Tetrahedron Letters, 2015, 56 (27), pp.4088-4092. ⟨10.1016/j.tetlet.2015.05.018⟩

Article dans une revue 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 et al.

European Journal of Organic Chemistry, 2015, 2015 (35), pp.7705-7717. ⟨10.1002/ejoc.201501129⟩

Article dans une revue istex 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 et al.

Organic Letters, 2015, organic letters, 17 (7), pp.1700-1713. ⟨10.1021/acs.orglett.5b00467⟩

Article dans une revue 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 et al.

Journal of Experimental Medicine, 2015, 212 (6), pp.723-740. ⟨10.1084/jem.20150002⟩

Article dans une revue hal-01160621v1
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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 et al.

Molecules, 2014, 19 (10), pp.15546-15571. ⟨10.3390/molecules191015546⟩

Article dans une revue hal-01141172v1

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 et al.

Tetrahedron, 2014, 70 (5541-5549), pp.5541-5549. ⟨10.1016/j.tet.2014.06.103⟩

Article dans une revue hal-01141181v1
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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 et al.

Molecules, 2014, 19 (10), pp.15411-15439. ⟨10.3390/molecules191015411⟩

Article dans une revue 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⟩

Article dans une revue hal-01141178v1

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 et al.

Journal of Organic Chemistry, 2013, 78 (16), pp.8191-8197. ⟨10.1021/jo401259w⟩

Article dans une revue hal-00997427v1

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 et al.

Bioorganic and Medicinal Chemistry Letters, 2013, 23 (24), pp.6784-6788. ⟨10.1016/j.bmcl.2013.10.019⟩

Article dans une revue istex hal-00997420v1

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 et al.

Journal of Heterocyclic Chemistry, 2013, 50 (5), pp.1187-1197. ⟨10.1002/jhet.1716⟩

Article dans une revue istex hal-01015485v1

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 et al.

Tetrahedron, 2013, 69 (15), pp.3182-3191. ⟨10.1016/j.tet.2013.02.066⟩

Article dans une revue istex hal-01015586v1

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⟩

Article dans une revue istex hal-01015451v1

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

Rémi Guillon , Fabrice Pagniez , Carine Picot , Damien Hédou , Alain Tonnerre et al.

ACS Medicinal Chemistry Letters, 2013, 4 (2), pp.288-292. ⟨10.1021/ml300429p⟩

Article dans une revue hal-01015468v1

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 et al.

European Journal of Organic Chemistry, 2013, 2013 (33), pp.7533-7545. ⟨10.1002/ejoc.201301014⟩

Article dans une revue istex hal-01015445v1

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 et al.

European Journal of Medicinal Chemistry, 2013, 59, pp.283-295. ⟨10.1016/j.ejmech.2012.11.030⟩

Article dans une revue istex 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⟩

Article dans une revue istex hal-01015472v1

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 et al.

European Journal of Medicinal Chemistry, 2012, 58, pp.171-183. ⟨10.1016/j.ejmech.2012.10.006⟩

Article dans une revue istex 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 et al.

Tetrahedron Letters, 2012, 53 (8), pp.944-947. ⟨10.1016/j.tetlet.2011.12.042⟩

Article dans une revue istex 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 et al.

Organic & Biomolecular Chemistry, 2012, 10 (25), pp.4916-4925. ⟨10.1039/c2ob25747e⟩

Article dans une revue 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 et al.

Bioorganic and Medicinal Chemistry Letters, 2012, 20 (8), pp.2614-2623. ⟨10.1016/j.bmc.2012.02.043⟩

Article dans une revue istex 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⟩

Article dans une revue istex hal-01018135v1

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 et al.

Chemical Communications, 2011, 47 (27), pp.7725-7727. ⟨10.1039/c1cc12099a⟩

Article dans une revue hal-01018301v1
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Structure of Pb<sup>2+</sup>/dCMP and Pb<sup>2+</sup>/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⟩

Article dans une revue hal-00619188v1

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 et al.

Tetrahedron, 2010, 66 (25), pp.4495-4502. ⟨10.1016/j.tet.2010.04.066⟩

Article dans une revue istex 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 et al.

Journal of Enzyme Inhibition and Medicinal Chemistry, 2010, 25 (2), pp.228-233. ⟨10.3109/14756360903169972⟩

Article dans une revue 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⟩

Article dans une revue istex hal-01019603v1

Synthesis and kinase inhibitory activity of novel substituted indigoids.

Anne Beauchard , Hélène Laborie , Hervé Rouillard , Olivier Lozach , Yoan Ferandin et al.

Bioorganic and Medicinal Chemistry, 2009, 17 (17), pp.6257-63. ⟨10.1016/j.bmc.2009.07.051⟩

Article dans une revue hal-00416031v1

Synthesis and kinase inhibitory activity of novel substituted indigoids

Anne Beauchard , Helene Laborie , Hervé Rouillard , Olivier Lozach , Yoan Ferandin et al.

Bioorganic and Medicinal Chemistry Letters, 2009, 17 (17), pp.6257-6263. ⟨10.1016/j.bmc.2009.07.051⟩

Article dans une revue hal-02357759v1

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 et al.

European Journal of Medicinal Chemistry, 2009, 44 (10), pp.3858-3865. ⟨10.1016/j.ejmech.2009.04.012⟩

Article dans une revue istex hal-01449310v1

Microwave-assisted synthesis of alpha-ethoxycarbamates

Alexandre Lumbroso , Floris Chevallier , Isabelle Beaudet , Jean-Paul Quintard , Thierry Besson et al.

Tetrahedron, 2009, 65 (45), pp.9180-9187. ⟨10.1016/j.tet.2009.09.023⟩

Article dans une revue 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 et al.

Journal of the American Chemical Society, 2008, 130 (45), pp.14916-14917. ⟨10.1021/ja805257v⟩

Article dans une revue istex hal-00467063v1

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 et al.

Journal of Enzyme Inhibition and Medicinal Chemistry, 2008, 19 (6), pp.467-473. ⟨10.1080/14756360412331280491⟩

Article dans une revue 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 et al.

Journal of Physical Chemistry A, 2008, 112 (48), pp.12393-12400. ⟨10.1021/jp806396t⟩

Article dans une revue hal-00368127v1

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⟩

Article dans une revue 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 et al.

European Journal of Medicinal Chemistry, 2008, 43 (7), pp.1469-1477. ⟨10.1016/j.ejmech.2007.09.020⟩

Article dans une revue istex hal-02357774v1

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

François Liger , Florence Popowycz , Thierry Besson , Laurent Picot , Carlos Galmarini et al.

Bioorganic and Medicinal Chemistry Letters, 2007, 15 (16), pp.5615-5619. ⟨10.1016/j.bmc.2007.05.033⟩

Article dans une revue istex hal-02357763v1

Synthesis of latonduine derivatives via intramolecular Heck coupling reaction

A. Putey , L. Joucla , L. Picot , Thierry Besson , B. Joseph.

Tetrahedron, 2007, pp.63, 867

Article dans une revue hal-00158714v1

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 et al.

Canadian Journal of Chemistry, 2007, 85 (11), pp.996-1005. ⟨10.1139/V07-112⟩

Article dans une revue 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⟩

Article dans une revue hal-02357738v1

Synthesis of novel 5-substituted indirubins as protein kinases inhibitors

Anne Beauchard , Yoan Ferandin , Stéphane Frère , Olivier Lozach , Mélina Blairvacq et al.

Bioorganic and Medicinal Chemistry, 2006, 14 (18), pp.6434-43. ⟨10.1016/j.bmc.2006.05.036⟩

Article dans une revue istex 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 et al.

Bioorganic and Medicinal Chemistry Letters, 2006, 16 (13), pp.3419-3423. ⟨10.1016/j.bmcl.2006.04.006⟩

Article dans une revue istex hal-02357746v1

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

Alexandra Testard , Laurent Picot , Olivier Lozach , Melina Blairvacq , Laurent Meijer et al.

Journal of Enzyme Inhibition and Medicinal Chemistry, 2005, 20 (6), pp.557-568. ⟨10.1080/14756360500212399⟩

Article dans une revue 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⟩

Article dans une revue 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⟩

Article dans une revue hal-02357727v1

Efficient solvent-free microwave phosphorylation of microcrystalline cellulose

Natalia Gospodinova , Axelle Grelard , Marc Jeannin , Gabrielle Chitanu , Adrian Carpov et al.

Green Chemistry, 2002, 4 (3), pp.220-222. ⟨10.1039/b200295g⟩

Article dans une revue istex 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⟩

Article dans une revue 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⟩

Article dans une revue 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 et al.

Earth and Planetary Science Letters, 1998, 147 (1-4), pp.83-92. ⟨10.1016/S0012-821X(97)00004-6⟩

Article dans une revue istex 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

Article dans une revue 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⟩

Article dans une revue hal-02357709v1

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⟩

Article dans une revue istex hal-02357768v1

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⟩

Article dans une revue istex hal-02889857v1

Biophysical and biological properties of newly synthesized dioxinocoumarin derivatives

Gabriella Csík , Györgyi Rontó , Silvano Nocentini , Simone Averbeck , Dietrich Averbeck et al.

Journal of Photochemistry and Photobiology B: Biology, 1994, 24 (2), pp.129-139. ⟨10.1016/1011-1344(94)07015-6⟩

Article dans une revue istex 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⟩

Article dans une revue istex 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⟩

Article dans une revue 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⟩

Article dans une revue hal-02357707v1

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 et al.

6th International Electronic Conference on Medicinal Chemistry, MDPI; Pharmaceuticals, Nov 2020, Sciforum.net, France. pp.7390, ⟨10.3390/ecmc2020-07390⟩

Communication dans un congrès hal-05335484v1

Synthesis of potential bioactive benzo-, pyrido-, or pyrazinothieno[3,2-d]pyrimidin- 4-amine analogs of MPC-6827

Yvonnick Loidreau , Marie-Renée Nourrisson , Corinne Fruit , Cécile Corbière , Pascal Marchand et al.

6th International Electronic Conference on Medicinal Chemistry, MDPI; Pharmaceuticals, Nov 2020, Sciforum.net, France. pp.7391, ⟨10.3390/ecmc2020-07391⟩

Communication dans un congrès hal-05335499v1

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

Communication dans un congrès 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 et al.

International Electronic Conference on Medicinal Chemistry (ECMC, 4, 2018), Jean-Jacques Vanden Eynde (coord.), Nov 2018, [online], Belgium. ⟨10.3390/ecmc-4-05580⟩

Communication dans un congrès 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

Communication dans un congrès hal-02384759v1

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⟩

Communication dans un congrès hal-02383887v1

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

Thierry Besson

Séminaire international, Katholieke Universiteit Leuven (KU), Jun 2017, Louvain, Belgium

Communication dans un congrès hal-02390455v1

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

Thierry Besson

Séminaire international, Universiteit Gent, Jun 2017, Gand, Belgium

Communication dans un congrès hal-02390460v1

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 et al.

International Electronic Conference on Medicinal Chemistry (ECMC, 2, 2016), Jean-Jacques Vanden Eynde (coord.), Nov 2016, [online], Belgium. ⟨10.3390/ecmc-2-A010⟩

Communication dans un congrès 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

Communication dans un congrès 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

Communication dans un congrès 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

Communication dans un congrès hal-02390779v1

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

Communication dans un congrès hal-02378695v1

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⟩

Communication dans un congrès 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

Communication dans un congrès hal-02390509v1

Microwave extraction of bioactive molecules

E. Destandau , S. Zubrzycki , C. Elfakir , Abdelhakim Elomri , Thierry Besson et al.

Cosmetic innovation days (COSMINNOV, 2013), Oct 2013, Orléans, France

Communication dans un congrès 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 et al.

35th congress of theoretical chemists of latin expression 35th QUITEL, Sep 2009, San Andres, Colombia

Communication dans un congrès 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

Communication dans un congrès hal-00275019v1