List of works - Thierry Besson

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

scientific article published on 16 May 2019

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.

scientific article published on 26 January 2015

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

scientific article

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

scientific article published on 07 June 2011

Biological Characterization of 8-Cyclopropyl-2-(pyridin-3-yl)thiazolo[5,4-f]quinazolin-9(8H)-one, a Promising Inhibitor of DYRK1A

scientific article published on 17 December 2019

Biophysical and biological properties of newly synthesized dioxinocoumarin derivatives. II. Dark and photoinduced effects on T7 phage, yeast and HeLa cells.

scientific article

Cytotoxic evaluation of sarcodifurines A and B, two novel dihydrofuroquinolines from Sarcomelicope follicularis (Rutaceae)

scientific article published on 01 October 2008

DYRK1A controls the transition from proliferation to quiescence during lymphoid development by destabilizing Cyclin D3

scientific article published on 25 May 2015

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

scientific article published in 2021

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

scientific article

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

scientific article

Development of Kinase Inhibitors via Metal-Catalyzed C⁻H Arylation of 8-Alkyl-thiazolo[5,4-]-quinazolin-9-ones Designed by Fragment-Growing Studies

article

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

scientific article published on 07 August 2013

Discovery of a novel broad-spectrum antifungal agent derived from albaconazole.

scientific article

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

scientific article published on 2 August 2017

Gas-phase structure of a pi-allyl-palladium complex: efficient infrared spectroscopy in a 7 T Fourier transform mass spectrometer.

scientific article

Influence of microwave irradiation on enzymatic properties: applications in enzyme chemistry.

scientific article published on October 2007

Influence of microwave radiation on free Candida antarctica lipase B activity and stability

article

Ligand-free Pd-catalyzed and copper-assisted C-H arylation of quinazolin-4-ones with aryl iodides under microwave heating

scientific article published on 17 March 2015

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

scientific article published on 19 August 2020

Microwave-assisted solid-phase synthesis of 5-carboxamido-N-acetyltryptamine derivatives

scientific article published on 01 August 2002

Microwave-assisted synthesis of bioactive quinazolines and quinazolinones.

scientific article published on December 2007

Microwave-assisted synthesis of galacto-oligosaccharides from lactose with immobilized beta-galactosidase from Kluyveromyces lactis.

scientific article published in April 2003

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.

scientific article published on 29 September 2007

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

scientific article published on 17 June 2016

Relieving Dyrk1a repression of MKL1 confers an adult-like phenotype to human infantile megakaryocytes

scientific article published in 2022

Room-Temperature Infrared Spectroscopy Combined with Mass Spectrometry Distinguishes Gas-Phase Protein Isomers

scientific article published on 01 January 2009

Stability improvement of immobilized Candida antarctica lipase B in an organic medium under microwave radiation

scientific article published on 10 March 2004

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

scientific article published on 22 May 2012

Synthesis and antiproliferative evaluation of 7-aminosubstituted pyrroloiminoquinone derivatives.

scientific article published in October 2000

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

scientific article

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.

scientific article published on 24 November 2012

Synthesis and cytotoxic evaluation of novel thiazolocarbazoles

Synthesis and cytotoxic evaluation of novel thiazolocarbazoles. Part III

Synthesis and kinase inhibitory activity of novel substituted indigoids.

scientific article

Synthesis of 2-Mercapto-(2-Oxoindolin-3-Ylidene)Acetonitriles from 3-(4-Chloro-5H-1,2,3-Dithiazol-5-Ylidene)Indolin-2-ones

scientific article published on 08 June 2018

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

scientific article

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

scientific article

Synthesis of novel 5-substituted indirubins as protein kinases inhibitors.

scientific article published on 8 June 2006

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

scientific article published on 03 March 2012

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.

scientific article

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

scientific article published on 27 April 2006

List of works by Thierry Besson

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

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.

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

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

Biological Characterization of 8-Cyclopropyl-2-(pyridin-3-yl)thiazolo[5,4-f]quinazolin-9(8H)-one, a Promising Inhibitor of DYRK1A

Biophysical and biological properties of newly synthesized dioxinocoumarin derivatives. II. Dark and photoinduced effects on T7 phage, yeast and HeLa cells.

Cytotoxic evaluation of sarcodifurines A and B, two novel dihydrofuroquinolines from Sarcomelicope follicularis (Rutaceae)

DYRK1A controls the transition from proliferation to quiescence during lymphoid development by destabilizing Cyclin D3

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

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

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

Development of Kinase Inhibitors via Metal-Catalyzed C⁻H Arylation of 8-Alkyl-thiazolo[5,4-]-quinazolin-9-ones Designed by Fragment-Growing Studies

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

Discovery of a novel broad-spectrum antifungal agent derived from albaconazole.

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

Gas-phase structure of a pi-allyl-palladium complex: efficient infrared spectroscopy in a 7 T Fourier transform mass spectrometer.

Influence of microwave irradiation on enzymatic properties: applications in enzyme chemistry.

Influence of microwave radiation on free Candida antarctica lipase B activity and stability

Ligand-free Pd-catalyzed and copper-assisted C-H arylation of quinazolin-4-ones with aryl iodides under microwave heating

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

Microwave-assisted solid-phase synthesis of 5-carboxamido-N-acetyltryptamine derivatives

Microwave-assisted synthesis of bioactive quinazolines and quinazolinones.

Microwave-assisted synthesis of galacto-oligosaccharides from lactose with immobilized beta-galactosidase from Kluyveromyces lactis.

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.

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

Relieving Dyrk1a repression of MKL1 confers an adult-like phenotype to human infantile megakaryocytes

Room-Temperature Infrared Spectroscopy Combined with Mass Spectrometry Distinguishes Gas-Phase Protein Isomers

Stability improvement of immobilized Candida antarctica lipase B in an organic medium under microwave radiation

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

Synthesis and antiproliferative evaluation of 7-aminosubstituted pyrroloiminoquinone derivatives.

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

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.

Synthesis and cytotoxic evaluation of novel thiazolocarbazoles

Synthesis and cytotoxic evaluation of novel thiazolocarbazoles. Part III

Synthesis and kinase inhibitory activity of novel substituted indigoids.

Synthesis of 2-Mercapto-(2-Oxoindolin-3-Ylidene)Acetonitriles from 3-(4-Chloro-5H-1,2,3-Dithiazol-5-Ylidene)Indolin-2-ones

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

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

Synthesis of novel 5-substituted indirubins as protein kinases inhibitors.

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

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.

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