List of works - Marc Nazaré

5-Aryl-2-(naphtha-1-yl)sulfonamido-thiazol-4(5H)-ones as clathrin inhibitors

scientific article

A General One-Pot Synthesis of 2H-Indazoles Using an Organophosphorus-Silane System.

scientific article published on 12 April 2018

A Palladium-Catalyzed Domino Reaction To Access 3-Amino-2H-indazoles from Hydrazines and 2-Halobenzonitriles

scientific article published on 01 September 2020

A flexible, palladium-catalyzed indole and azaindole synthesis by direct annulation of chloroanilines and chloroaminopyridines with ketones.

scientific article published in August 2004

A general and mild domino approach to substituted 1-aminoindoles

scientific article published on 12 November 2010

A general and mild palladium-catalyzed domino reaction for the synthesis of 2H-indazoles

scientific article published on 01 January 2009

A new highly thyrotropin receptor-selective small molecule antagonist with potential for the treatment of Graves' orbitopathy

article

A novel nitroreductase-enhanced MRI contrast agent and its potential application in bacterial imaging.

scientific article published on 6 December 2017

A pharmacological master key mechanism that unlocks the selectivity filter gate in K+ channels ⬇️

scientific article published on 01 February 2019

Allosteric inhibition of a mammalian lectin

scientific article published on 24 October 2018

CellFy: A Cell-Based Fragment Screen against C-Type Lectins

scientific article published on 03 December 2018

Chemical fragment arrays for rapid druggability assessment.

scientific article published on 18 February 2016

DOTAM derivatives as active cartilage-targeting drug carriers for the treatment of osteoarthritis

scientific article published on 12 February 2015

Designed nanomolar small-molecule inhibitors of Ena/VASP EVH1 interaction impair invasion and extravasation of breast cancer cells

scientific article published on 12 November 2020

Development of a 1,2,4-Triazole-Based Lead Tankyrase Inhibitor: Part II

scientific article published on 08 December 2021

Direct Experimental Evidence for Halogen-Aryl π Interactions in Solution from Molecular Torsion Balances.

scientific article published on 28 April 2017

Discovery of N-[4-(1H-Pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides as Highly Active and Selective SGK1 Inhibitors

scientific article published on 23 October 2014

Discovery of a Novel Series of Tankyrase Inhibitors by a Hybridization Approach

scientific article published on 20 November 2017

EU-OPENSCREEN: A Novel Collaborative Approach to Facilitate Chemical Biology

scientific article published on 07 January 2019

Efficient enantioselective synthesis of a β-hydroxyepoxide building block for the construction of macrocyclic natural products

Enantiospecific synthesis of the (9S,18R)-diastereomer of the leukocyte adhesion inhibitor cyclamenol A.

scientific article

Evidence for C-Cl/C-Br...pi interactions as an important contribution to protein-ligand binding affinity.

scientific article published in January 2009

Factor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of neutral P1 substituents.

scientific article

Fragment deconstruction of small, potent factor Xa inhibitors: exploring the superadditivity energetics of fragment linking in protein-ligand complexes

scientific article

From Pyrazolones to Azaindoles: Evolution of Active-Site SHP2 Inhibitors Based on Scaffold Hopping and Bioisosteric Replacement

scientific article published on 19 November 2020

Identification and Characterization of a Single High-Affinity Fatty Acid Binding Site in Human Serum Albumin

scientific article published on 28 November 2017

Identification of a Novel Benzimidazole Pyrazolone Scaffold That Inhibits KDM4 Lysine Demethylases and Reduces Proliferation of Prostate Cancer Cells

scientific article published on 27 March 2017

Identification of high-affinity P2Y₁₂ antagonists based on a phenylpyrazole glutamic acid piperazine backbone

scientific article

Loss of Ptpn11 (Shp2) drives satellite cells into quiescence

scientific article published on 2 May 2017

Modulation of Hexadecyl-LPA-Mediated Activation of Mast Cells and Microglia by a Chemical Probe for LPA5.

scientific article published on 26 January 2016

Mutant KRAS-driven cancers depend on PTPN11/SHP2 phosphatase.

scientific article

N-[6-(4-butanoyl-5-methyl-1H-pyrazol-1-yl)pyridazin-3-yl]-5-chloro-1-[2-(4-methylpiperazin-1-yl)-2-oxoethyl]-1H-indole-3-carboxamide (SAR216471), a novel intravenous and oral, reversible, and directly acting P2Y12 antagonist

scientific article published on 25 August 2014

Organophosphorus-mediated N-N bond formation: facile access to 3-amino-2H-indazoles

scientific article

Probing 2H-Indazoles as Templates for SGK1, Tie2, and SRC Kinase Inhibitors

scientific article published on 31 July 2019

Probing the subpockets of factor Xa reveals two binding modes for inhibitors based on a 2-carboxyindole scaffold: a study combining structure-activity relationship and X-ray crystallography.

scientific article published in July 2005

Rapid Synthesis of γ-Halide/Pseudohalide-Substituted Cyanine Sensors with Programmed Generation of Singlet Oxygen

scientific article published on 12 March 2019

Revealing cytotoxic substructures in molecules using deep learning

scientific article published on 16 April 2020

Selective non-lipid modulator of LPA5 activity in human platelets.

scientific article

Small-Molecule Lysophosphatidic Acid Receptor 5 (LPAR5) Antagonists: Versatile Pharmacological Tools to Regulate Inflammatory Signaling in BV-2 Microglia Cells

scientific article published on 29 November 2019

Synthesis of the (9S,18R) Diastereomer of Cyclamenol A This research was supported by the Bayer AG and the Fonds der chemischen Industrie

scientific article published on 01 March 2000

Synthesis of the (9S,18R)-seco acid of the leukocyte adhesion inhibitor cyclamenol A

Temperature dependence of cross-effect dynamic nuclear polarization in rotating solids: advantages of elevated temperatures

scientific article published on 28 October 2016

Tractable synthesis of multipurpose screening compounds with under-represented molecular features for an open access screening platform

scientific article

Use of a sequential high throughput screening assay to identify novel inhibitors of the eukaryotic SRP-Sec61 targeting/translocation pathway

scientific article published in PLoS ONE

Weizhouochrones: Gorgonian-Derived Symmetric Dimers and Their Structure Elucidation Using Anisotropic NMR Combined with DP4+ Probability and CASE-3D

scientific article published in 2022

visualization of osteoarthritic hypertrophic lesions

scientific article published on 12 August 2015

List of works by Marc Nazaré

5-Aryl-2-(naphtha-1-yl)sulfonamido-thiazol-4(5H)-ones as clathrin inhibitors

A General One-Pot Synthesis of 2H-Indazoles Using an Organophosphorus-Silane System.

A Palladium-Catalyzed Domino Reaction To Access 3-Amino-2H-indazoles from Hydrazines and 2-Halobenzonitriles

A flexible, palladium-catalyzed indole and azaindole synthesis by direct annulation of chloroanilines and chloroaminopyridines with ketones.

A general and mild domino approach to substituted 1-aminoindoles

A general and mild palladium-catalyzed domino reaction for the synthesis of 2H-indazoles

A new highly thyrotropin receptor-selective small molecule antagonist with potential for the treatment of Graves' orbitopathy

A novel nitroreductase-enhanced MRI contrast agent and its potential application in bacterial imaging.

A pharmacological master key mechanism that unlocks the selectivity filter gate in K+ channels ⬇️

Allosteric inhibition of a mammalian lectin

CellFy: A Cell-Based Fragment Screen against C-Type Lectins

Chemical fragment arrays for rapid druggability assessment.

DOTAM derivatives as active cartilage-targeting drug carriers for the treatment of osteoarthritis

Designed nanomolar small-molecule inhibitors of Ena/VASP EVH1 interaction impair invasion and extravasation of breast cancer cells

Development of a 1,2,4-Triazole-Based Lead Tankyrase Inhibitor: Part II

Direct Experimental Evidence for Halogen-Aryl π Interactions in Solution from Molecular Torsion Balances.

Discovery of N-[4-(1H-Pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides as Highly Active and Selective SGK1 Inhibitors

Discovery of a Novel Series of Tankyrase Inhibitors by a Hybridization Approach

EU-OPENSCREEN: A Novel Collaborative Approach to Facilitate Chemical Biology

Efficient enantioselective synthesis of a β-hydroxyepoxide building block for the construction of macrocyclic natural products

Enantiospecific synthesis of the (9S,18R)-diastereomer of the leukocyte adhesion inhibitor cyclamenol A.

Evidence for C-Cl/C-Br...pi interactions as an important contribution to protein-ligand binding affinity.

Factor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of neutral P1 substituents.

Fragment deconstruction of small, potent factor Xa inhibitors: exploring the superadditivity energetics of fragment linking in protein-ligand complexes

From Pyrazolones to Azaindoles: Evolution of Active-Site SHP2 Inhibitors Based on Scaffold Hopping and Bioisosteric Replacement

Identification and Characterization of a Single High-Affinity Fatty Acid Binding Site in Human Serum Albumin

Identification of a Novel Benzimidazole Pyrazolone Scaffold That Inhibits KDM4 Lysine Demethylases and Reduces Proliferation of Prostate Cancer Cells

Identification of high-affinity P2Y₁₂ antagonists based on a phenylpyrazole glutamic acid piperazine backbone

Loss of Ptpn11 (Shp2) drives satellite cells into quiescence

Modulation of Hexadecyl-LPA-Mediated Activation of Mast Cells and Microglia by a Chemical Probe for LPA5.

Mutant KRAS-driven cancers depend on PTPN11/SHP2 phosphatase.

N-[6-(4-butanoyl-5-methyl-1H-pyrazol-1-yl)pyridazin-3-yl]-5-chloro-1-[2-(4-methylpiperazin-1-yl)-2-oxoethyl]-1H-indole-3-carboxamide (SAR216471), a novel intravenous and oral, reversible, and directly acting P2Y12 antagonist

Organophosphorus-mediated N-N bond formation: facile access to 3-amino-2H-indazoles

Probing 2H-Indazoles as Templates for SGK1, Tie2, and SRC Kinase Inhibitors

Probing the subpockets of factor Xa reveals two binding modes for inhibitors based on a 2-carboxyindole scaffold: a study combining structure-activity relationship and X-ray crystallography.

Rapid Synthesis of γ-Halide/Pseudohalide-Substituted Cyanine Sensors with Programmed Generation of Singlet Oxygen

Revealing cytotoxic substructures in molecules using deep learning

Selective non-lipid modulator of LPA5 activity in human platelets.

Small-Molecule Lysophosphatidic Acid Receptor 5 (LPAR5) Antagonists: Versatile Pharmacological Tools to Regulate Inflammatory Signaling in BV-2 Microglia Cells

Synthesis of the (9S,18R) Diastereomer of Cyclamenol A This research was supported by the Bayer AG and the Fonds der chemischen Industrie

Synthesis of the (9S,18R)-seco acid of the leukocyte adhesion inhibitor cyclamenol A

Temperature dependence of cross-effect dynamic nuclear polarization in rotating solids: advantages of elevated temperatures

Tractable synthesis of multipurpose screening compounds with under-represented molecular features for an open access screening platform

Use of a sequential high throughput screening assay to identify novel inhibitors of the eukaryotic SRP-Sec61 targeting/translocation pathway

Weizhouochrones: Gorgonian-Derived Symmetric Dimers and Their Structure Elucidation Using Anisotropic NMR Combined with DP4+ Probability and CASE-3D

visualization of osteoarthritic hypertrophic lesions