List of works - Raphaël Frédérick

1-(2-Hydroxybenzoyl)-thiosemicarbazides are promising antimicrobial agents targeting d-alanine-d-alanine ligase in bacterio

scientific article published on 28 September 2018

31ièmes Journées Franco-Belges de Pharmacochimie: Meeting Report

scientific article

Anti-alcohol abuse drug disulfiram inhibits human PHGDH via disruption of its active tetrameric form through a specific cysteine oxidation

scientific article published on 18 March 2019

Arginase Structure and Inhibition: Catalytic Site Plasticity Reveals New Modulation Possibilities

scientific article published on 19 October 2017

Challenges and Opportunities in the Development of Serine Synthetic Pathway Inhibitors for Cancer Therapy

scientific article published on 13 December 2016

Computational tools for in silico fragment-based drug design.

scientific article

Coumarin and isocoumarin as serine protease inhibitors.

scientific article

Current state on tryptophan 2,3-dioxygenase inhibitors: a patent review

scientific article published on 16 January 2019

Design, solid-phase synthesis, and biological evaluation of novel 1,5-diarylpyrrole-3-carboxamides as carbonic anhydrase IX inhibitors.

scientific article

Discovery and preliminary SARs of keto-indoles as novel indoleamine 2,3-dioxygenase (IDO) inhibitors ⬇️

scientific article published on February 26, 2011

Discovery of pyrazolo[1,5-a]pyridines as p110α-selective PI3 kinase inhibitors.

scientific article

Indol-2-yl ethanones as novel indoleamine 2,3-dioxygenase (IDO) inhibitors.

scientific article published on 16 December 2010

Indoleamine 2,3-dioxygenase inhibitors: a patent review (2008 - 2012).

scientific article published on 30 August 2013

Indoleamine 2,3-dioxygenase inhibitory activity of derivatives of marine alkaloid tsitsikammamine A.

scientific article published on 22 November 2012

Interrogating the Lactate Dehydrogenase Tetramerization Site Using (Stapled) Peptides

scientific article published on 06 April 2020

Intestinal Sucrase as a Novel Target Contributing to the Regulation of Glycemia by Prebiotics

scientific article

Investigation of mechanism-based thrombin inhibitors: Implications of a highly conserved water molecule for the binding of coumarins within the S pocket.

scientific article published on 18 January 2006

Lactate Dehydrogenase B Controls Lysosome Activity and Autophagy in Cancer

scientific journal article

Ligand-based and structure-based virtual screening to identify carbonic anhydrase IX inhibitors

scientific article published on 06 December 2008

Mechanism-based thrombin inhibitors: design, synthesis, and molecular docking of a new selective 2-oxo-2H-1-benzopyran derivative

scientific article published on 20 June 2007

Modulators of the coagulation cascade: focus and recent advances in inhibitors of tissue factor, factor VIIa and their complex.

scientific article

NF-kappaB inducing kinase (NIK) inhibitors: identification of new scaffolds using virtual screening.

scientific article published on 8 June 2010

New selective carbonic anhydrase IX inhibitors: synthesis and pharmacological evaluation of diarylpyrazole-benzenesulfonamides.

scientific article

Novel pyrazolo[1,5-a]pyridines as p110α-selective PI3 kinase inhibitors: Exploring the benzenesulfonohydrazide SAR ⬇️

scientific article published on November 25, 2011

Novel trisubstituted harmine derivatives with original in vitro anticancer activity

scientific article

Olaparib Is a Mitochondrial Complex I Inhibitor That Kills Temozolomide-Resistant Human Glioblastoma Cells

scientific article published in 2021

Phosphoinositide-3-kinase (PI3K) inhibitors: identification of new scaffolds using virtual screening.

scientific article

Pyrazolo[4,3-c]isoquinolines as potential inhibitors of NF-kappaB activation

scientific article published on 21 January 2010

Radiosynthesis and validation of (±)-[18F]-3-fluoro-2-hydroxypropionate ([18F]-FLac) as a PET tracer of lactate to monitor MCT1-dependent lactate uptake in tumors

scientific article

Reversal of tumoral immune resistance by inhibition of tryptophan 2,3-dioxygenase

scientific article

Synthesis and In Vitro Evaluation of Polyethylene Glycol-Paclitaxel Conjugates for Lung Cancer Therapy

scientific article published on 16 March 2016

Synthesis and biological evaluation of di-aryl urea derivatives as c-Kit inhibitors.

scientific article

Synthesis and biological evaluation of novel analogues of the pan class I phosphatidylinositol 3-kinase (PI3K) inhibitor 2-(difluoromethyl)-1-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]-1H-benzimidazole (ZSTK474).

scientific article

Synthesis and evaluation of β-carboline derivatives as potential monoamine oxidase inhibitors

scientific article published on 25 November 2010

Synthesis and inhibition study of monoamine oxidase, indoleamine 2,3-dioxygenase and tryptophan 2,3-dioxygenase by 3,8-substituted 5H-indeno[1,2-c]pyridazin-5-one derivatives

scientific article published on 08 October 2011

Synthesis, biological evaluation and molecular modelling of sulfonohydrazides as selective PI3K p110alpha inhibitors.

scientific article published on 4 September 2007

Synthesis, crystal structures and electronic properties of isomers of chloro-pyridinylvinyl-1H-indoles ⬇️

scientific article published on May 3, 2012

Synthesis, evaluation and structure-activity relationship of new 3-carboxamide coumarins as FXIIa inhibitors

scientific article published on 16 January 2016

Synthesis, structural reassignment, and biological activity of type B MAO inhibitors based on the 5H-indeno[1,2-c]pyridazin-5-one core

scientific article (publication date: 15 June 2006)

Thiosemicarbazide, a fragment with promising indolamine-2,3-dioxygenase (IDO) inhibition properties

scientific article published on 15 May 2014

Three 5H-indeno[1,2-c]pyridazin-5-one derivatives, potent type-B monoamine oxidase inhibitors.

scientific article published on 11 August 2004

Tryptophan 2,3-Dioxygenase (TDO) Inhibitors. 3-(2-(Pyridyl)ethenyl)indoles as Potential Anticancer Immunomodulators ⬇️

scientific article published on July 18, 2011

α-Ketothioamide Derivatives: A Promising Tool to Interrogate Phosphoglycerate Dehydrogenase (PHGDH).

scientific article published on 13 January 2017

List of works by Raphaël Frédérick

1-(2-Hydroxybenzoyl)-thiosemicarbazides are promising antimicrobial agents targeting d-alanine-d-alanine ligase in bacterio

31ièmes Journées Franco-Belges de Pharmacochimie: Meeting Report

Anti-alcohol abuse drug disulfiram inhibits human PHGDH via disruption of its active tetrameric form through a specific cysteine oxidation

Arginase Structure and Inhibition: Catalytic Site Plasticity Reveals New Modulation Possibilities

Challenges and Opportunities in the Development of Serine Synthetic Pathway Inhibitors for Cancer Therapy

Computational tools for in silico fragment-based drug design.

Coumarin and isocoumarin as serine protease inhibitors.

Current state on tryptophan 2,3-dioxygenase inhibitors: a patent review

Design, solid-phase synthesis, and biological evaluation of novel 1,5-diarylpyrrole-3-carboxamides as carbonic anhydrase IX inhibitors.

Discovery and preliminary SARs of keto-indoles as novel indoleamine 2,3-dioxygenase (IDO) inhibitors ⬇️

Discovery of pyrazolo[1,5-a]pyridines as p110α-selective PI3 kinase inhibitors.

Indol-2-yl ethanones as novel indoleamine 2,3-dioxygenase (IDO) inhibitors.

Indoleamine 2,3-dioxygenase inhibitors: a patent review (2008 - 2012).

Indoleamine 2,3-dioxygenase inhibitory activity of derivatives of marine alkaloid tsitsikammamine A.

Interrogating the Lactate Dehydrogenase Tetramerization Site Using (Stapled) Peptides

Intestinal Sucrase as a Novel Target Contributing to the Regulation of Glycemia by Prebiotics

Investigation of mechanism-based thrombin inhibitors: Implications of a highly conserved water molecule for the binding of coumarins within the S pocket.

Lactate Dehydrogenase B Controls Lysosome Activity and Autophagy in Cancer

Ligand-based and structure-based virtual screening to identify carbonic anhydrase IX inhibitors

Mechanism-based thrombin inhibitors: design, synthesis, and molecular docking of a new selective 2-oxo-2H-1-benzopyran derivative

Modulators of the coagulation cascade: focus and recent advances in inhibitors of tissue factor, factor VIIa and their complex.

NF-kappaB inducing kinase (NIK) inhibitors: identification of new scaffolds using virtual screening.

New selective carbonic anhydrase IX inhibitors: synthesis and pharmacological evaluation of diarylpyrazole-benzenesulfonamides.

Novel pyrazolo[1,5-a]pyridines as p110α-selective PI3 kinase inhibitors: Exploring the benzenesulfonohydrazide SAR ⬇️

Novel trisubstituted harmine derivatives with original in vitro anticancer activity

Olaparib Is a Mitochondrial Complex I Inhibitor That Kills Temozolomide-Resistant Human Glioblastoma Cells

Phosphoinositide-3-kinase (PI3K) inhibitors: identification of new scaffolds using virtual screening.

Pyrazolo[4,3-c]isoquinolines as potential inhibitors of NF-kappaB activation

Radiosynthesis and validation of (±)-[18F]-3-fluoro-2-hydroxypropionate ([18F]-FLac) as a PET tracer of lactate to monitor MCT1-dependent lactate uptake in tumors

Reversal of tumoral immune resistance by inhibition of tryptophan 2,3-dioxygenase

Synthesis and In Vitro Evaluation of Polyethylene Glycol-Paclitaxel Conjugates for Lung Cancer Therapy

Synthesis and biological evaluation of di-aryl urea derivatives as c-Kit inhibitors.

Synthesis and biological evaluation of novel analogues of the pan class I phosphatidylinositol 3-kinase (PI3K) inhibitor 2-(difluoromethyl)-1-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]-1H-benzimidazole (ZSTK474).

Synthesis and evaluation of β-carboline derivatives as potential monoamine oxidase inhibitors

Synthesis and inhibition study of monoamine oxidase, indoleamine 2,3-dioxygenase and tryptophan 2,3-dioxygenase by 3,8-substituted 5H-indeno[1,2-c]pyridazin-5-one derivatives

Synthesis, biological evaluation and molecular modelling of sulfonohydrazides as selective PI3K p110alpha inhibitors.

Synthesis, crystal structures and electronic properties of isomers of chloro-pyridinylvinyl-1H-indoles ⬇️

Synthesis, evaluation and structure-activity relationship of new 3-carboxamide coumarins as FXIIa inhibitors

Synthesis, structural reassignment, and biological activity of type B MAO inhibitors based on the 5H-indeno[1,2-c]pyridazin-5-one core

Thiosemicarbazide, a fragment with promising indolamine-2,3-dioxygenase (IDO) inhibition properties

Three 5H-indeno[1,2-c]pyridazin-5-one derivatives, potent type-B monoamine oxidase inhibitors.

Tryptophan 2,3-Dioxygenase (TDO) Inhibitors. 3-(2-(Pyridyl)ethenyl)indoles as Potential Anticancer Immunomodulators ⬇️

α-Ketothioamide Derivatives: A Promising Tool to Interrogate Phosphoglycerate Dehydrogenase (PHGDH).