L. Meerpoel

发表

Synthesis and Reactivity of Spirocarbocycles as Scaffolds for Nucleoside Analogues.

F. De Proft, V. Pande, Jonas Verhoeven, 2020, The Journal of organic chemistry.

Copper-catalysed amidation of 2-chloro-pyridines

I. Stansfield, L. Meerpoel, J. Cossy, 2013 .

FEP+ calculations predict a stereochemical SAR switch for first-in-class indoline NIK inhibitors for multiple myeloma

E. Jacoby, G. Hynd, I. Stansfield, 2020 .

Ruthenium-catalyzed α-(hetero)arylation of saturated cyclic amines: reaction scope and mechanism.

B. Maes, L. Meerpoel, W. Herrebout, 2013, Chemistry.

Direct α-functionalization of saturated cyclic amines.

B. Maes, L. Meerpoel, Nicolas Lefèvre, 2012, Chemistry.

The Novel Azole R126638 Is a Selective Inhibitor of Ergosterol Synthesis in Candida albicans, Trichophyton spp., and Microsporum canis

L. Meerpoel, J. Ausma, F. Odds, 2004, Antimicrobial Agents and Chemotherapy.

Design and synthesis of a series of bioavailable fatty acid synthase (FASN) KR domain inhibitors for cancer therapy.

Tianbao Lu, G. Bignan, M. Cummings, 2018, Bioorganic & medicinal chemistry letters.

A fungicidal piperazine-1-carboxamidine induces mitochondrial fission-dependent apoptosis in yeast.

L. Meerpoel, B. Cammue, K. Thevissen, 2010, FEMS yeast research.

Abstract DDT02-04: A novel PRMT5 inhibitor with potent in vitro and in vivo activity in preclinical lung cancer models

Italo Poggesi, Vineet Pande, James P. Edwards, 2017 .

Design and Synthesis of a Series of Piperazine‐1‐carboxamidine Derivatives with Antifungal Activity Resulting from Accumulation of Endogenous Reactive Oxygen Species

J. Heeres, L. Meerpoel, J. Pastor, 2009, ChemMedChem.

Triphenylphosphine: a catalyst for the synthesis of C-aryl furanosides from furanosyl halides

I. Stansfield, L. Meerpoel, J. Cossy, 2014 .

Cobalt-catalyzed diastereoselective synthesis of C-furanosides. Total synthesis of (-)-isoaltholactone.

I. Stansfield, L. Meerpoel, J. Cossy, 2013, The Journal of organic chemistry.

Abstract 801: Sensitivity of cell lines to Fatty Acid Synthase inhibitors depends on the lipid content in the cellular environment

Yolanda T. Chong, Tianbao Lu, G. Bignan, 2014 .

Pyrrolo[1,2-a][1,4]benzodiazepine: a novel class of non-azole anti-dermatophyte anti-fungal agents.

L. Meerpoel, J. van Gestel, P. Marichal, 2005, Bioorganic & medicinal chemistry letters.

A Chemical Probe for the Methyl Transferase PRMT5 with a Novel Binding Mode.

V. Pande, D. Brehmer, M. Paradé, 2020, ACS medicinal chemistry letters.

Fragment-based discovery of type I inhibitors of maternal embryonic leucine zipper kinase.

F. Sommen, A. Sharff, V. Berdini, 2015, ACS medicinal chemistry letters.

Discovery and Pharmacological Characterization of JNJ-64619178, a Novel Small-Molecule Inhibitor of PRMT5 with Potent Antitumor Activity

Bie M. P. Verbist, U. Philippar, T. Graubert, 2021, Molecular Cancer Therapeutics.

Face Selectivity of the Diels-Alder Additions and Cheletropic Additions of Sulfur-Dioxide to 2-Vinyl-7-Oxabicyclo[2.2.1]Hept-2-Ene Derivatives

P. Vogel, L. Meerpoel, B. Deguin, 1994 .

Removal of the pyridine directing group from α-substituted N-(pyridin-2-yl)piperidines obtained via directed Ru-catalyzed sp3 C-H functionalization.

Christophe M. L. Vande Velde, P. Bultinck, B. Maes, 2013, The Journal of organic chemistry.

C-2 arylation of piperidines through directed transition-metal-catalyzed sp3 C-H activation.

B. Maes, L. Meerpoel, W. Herrebout, 2010, Chemistry.

In Vitro and In Vivo Activities of the Novel Azole Antifungal Agent R126638

J. Heeres, L. Meerpoel, J. Ausma, 2004, Antimicrobial Agents and Chemotherapy.

Organic glasses with tunable liquid-crystalline order through kinetic arrest of end-over-end rotation: the case of saperconazole.

Lian Yu, R. Richert, L. Meerpoel, 2020, Soft matter.

Diastereoselective Synthesis of trans‐2,3‐Diaryl(heteroaryl)‐3,6‐dihydropyrans by an Allylboration/Ring‐Closing‐Metathesis Sequence

I. Stansfield, Pierre-Antoine Nocquet, L. Meerpoel, 2017 .

Synthesis of 3,5-dihalogeno-2H-1,4-oxazin-2-ones from cyanohydrines

L. Meerpoel, G. Hoornaert, 1989 .

Functionalisation in position 3 of 3,5-dichloro-2H-1,4-oxazin-2-ones

L. Meerpoel, G. Hoornaert, K. V. Aken, 1992 .

The Synthesis of 3-Functionalized 5-chloro-6-methyl-2H-1,4-oxazin-2-ones and of pyridines from cycloaddition-elimination reactions with substituted acetylenic compounds.

L. Meerpoel, G. Hoornaert, G. Deroover, 1994 .

Diels-Alder Reactions of 6-Alkyl-3,5-dichloro-2H-1,4-oxazin-2-ones with Alkynes: Synthesis of 3,5-Disubstituted 2,6-Dichloropyridines.

L. Meerpoel, G. Hoornaert, G. Deroover, 1992 .

Synthesis of 6-methoxy- and 6-chloro-2(1H)-pyridinone acyclo-C-Nucleosides from 2H-1,4-oxazin-2-ones.

L. Meerpoel, G. Hoornaert, G. Joly, 1993 .

Cycloaddition of olefinic compounds to 2H-1,4-oxazin-2-ones : synthesis of 2-oxa-5-azabicyclo[2.2.2]oct-5-en-3-ones

L. Meerpoel, S. Toppet, G. Hoornaert, 1992 .

Diels-Alder Reactions of 6-Alkyl-3,5-dichloro-2H-1,4-oxazin-2-ones with Alkynes: Synthesis of 3,5-Disubstituted 2,6-Dichloropyridines

L. Meerpoel, G. Hoornaert, G. Deroover, 1991 .

A general-synthesis of 3,5-dihalo-2h-1,4-oxazin-2-ones from cyanohydrins

L. Meerpoel, G. Hoornaert, 1990 .

Discovery of JNJ-63576253, a Next-Generation Androgen Receptor Antagonist Active Against Wild-Type and Clinically Relevant Ligand Binding Domain Mutations in Metastatic Castration-Resistant Prostate Cancer

Yolanda T. Chong, T. Bush, G. Bignan, 2021, Molecular Cancer Therapeutics.

Title: Discovery of JNJ-63576253, a next-generation androgen receptor antagonist active against wild- type and clinically-relevant ligand binding domain mutations in metastatic castration-resistant prostate cancer (mCRPC) Running Title: Discovery of JNJ-63576253, a next-generation AR antagonist

Yolanda T. Chong, T. Bush, G. Bignan, 2021 .

Minisci-Photoredox-Mediated α-Heteroarylation of N-Protected Secondary Amines: Remarkable Selectivity of Azetidines.

J. Edwards, H. Beucher, L. Meerpoel, 2018, Organic letters.

Synthesis of Novel Isothiazole and Isothiazolo[4,5-d] Pyrimidine Analogues of the Natural C-Nucleosides Pyrazofurin and the Formycins

L. Meerpoel, S. Toppet, G. Hoornaert, 1994 .

Synthesis of substituted indenones and indanones by a Suzuki-Miyaura coupling/acid-promoted cyclisation sequence.

I. Stansfield, L. Meerpoel, A. Corbu, 2014, Organic & biomolecular chemistry.

Iron-Catalyzed Synthesis of Sulfur-Containing Heterocycles.

I. Stansfield, L. Meerpoel, J. Cossy, 2017, The Journal of organic chemistry.

Synthesis and orthogonal functionalization of oxazolo[5',4':4,5]pyrano[2,3-b]pyridine by intra- and intermolecular Pd-catalyzed direct C-H bond heteroarylation.

L. Meerpoel, C. Hoarau, O. Querolle, 2016, Organic & biomolecular chemistry.

Cycloaddition of 3-Amino-5-chloro-2(1H)-pyrazinones and Olefins: Ring Transformation into 3-Amino- or 6-Cyano-Substituted 2-Pyridinone Systems

L. Meerpoel, G. Hoornaert, S. Vandenberghe, 1996 .

Iron-Catalyzed Synthesis of C2 Aryl- and N-Heteroaryl-Substituted Tetrahydropyrans.

L. Meerpoel, J. Cossy, A. Guérinot, 2015, The Journal of organic chemistry.

Access to Silylated Pyrazole Derivatives by Palladium-Catalyzed C-H Activation of a TMS group.

L. Meerpoel, J. Maddaluno, M. Durandetti, 2016, Chemistry.

Intramolecular sila-Matteson rearrangement: a general access to silylated heterocycles.

L. Meerpoel, L. van Hijfte, J. Maddaluno, 2012, Organic letters.

An approach to acyclo-1-deazathymidine c-nucleosides via 3,5-dichloro-6-methyl-2H-1,4-oxazin-2-one.

L. Meerpoel, S. Toppet, F. Compernolle, 1991 .

Two-step one-pot synthesis of benzoannulated spiroacetals by Suzuki-Miyaura coupling/acid-catalyzed spiroacetalization.

P. Bonnet, I. Stansfield, L. Meerpoel, 2012, Organic letters.

Homochiral matching in the Diels-Alder cyclodimerization of 2-vinyl-7-oxabicyclo[2.2.1]hept-2-ene derivatives

P. Vogel, L. Meerpoel, J. Ancerewicz, 1994 .

Anionic access to silylated and germylated binuclear heterocycles.

L. Meerpoel, J. Maddaluno, M. Durandetti, 2014, Chemistry.

The role of the alcohol and carboxylic acid in directed ruthenium-catalyzed C(sp3)-H α-alkylation of cyclic amines.

B. Maes, L. Meerpoel, H. Prokopcová, 2012, Chemistry.

Tandem Suzuki-Miyaura coupling/acid-catalyzed cyclization between vinyl ether boronates and vinyl halides: a concise approach to polysubstituted furans.

I. Stansfield, L. Meerpoel, A. Corbu, 2013, Organic letters.

Diastereoselective Metal-Catalyzed Synthesis ofC-Aryl andC-Vinyl Glycosides

P. Bonnet, I. Stansfield, L. Meerpoel, 2012 .

Diastereoselective metal-catalyzed synthesis of C-aryl and C-vinyl glycosides.

P. Bonnet, I. Stansfield, L. Meerpoel, 2012, Angewandte Chemie.

Synthesis and transformations of pyrrolo[1,2-a][1,3,5]-triazines

Jonas Verhoeven, L. Meerpoel, J. Thuring, 2018, Tetrahedron Letters.

C-Glycosides and C-disaccharide precursors through carbonylative Stille coupling reactions

P. Vogel, L. Meerpoel, V. Jeanneret, 1997 .

Directed Ruthenium‐Catalyzed C(sp3) ? H α‐Alkylation of Cyclic Amines Using Dioxolane‐Protected Alkenones

B. Maes, L. Meerpoel, A. A. Kulago, 2014 .

Synthesis and in vitro and in vivo Antifungal Activity of the Hydroxy Metabolites of Saperconazole

J. Heeres, M. Oris, L. Meerpoel, 2010, ChemMedChem.

Conazoles

J. Heeres, P. Lewi, L. Meerpoel, 2010, Molecules.

Synthesis and in vitro and in vivo structure-activity relationships of novel antifungal triazoles for dermatology.

J. Heeres, M. Oris, L. Meerpoel, 2005, Journal of medicinal chemistry.

In Vitro and In Vivo Activities of the Novel Azole Antifungal Agent R 126638

J. Heeres, L. Meerpoel, J. Ausma, 2004 .

Pyrrolo[1,2-α][1,4]benzodiazepines show potent in vitro antifungal activity and significant in vivo efficacy in a Microsporum canis dermatitis model in guinea pigs.

L. Maes, L. Meerpoel, P. Cos, 2014, The Journal of antimicrobial chemotherapy.

Preparation of 4'-Spirocyclobutyl Nucleoside Analogues as Novel and Versatile Adenosine Scaffolds.

V. Pande, Jonas Verhoeven, Weimei Sun, 2019, Chemistry.

Regio- and Stereoselective Synthesis of C-4' Spirocyclobutyl Ribofuranose Scaffolds and Their Use as Biologically Active Nucleoside Analogues.

Jonas Verhoeven, L. Meerpoel, J. Thuring, 2021, Organic letters.

Stereodivergent Synthesis of Biologically Active Spironucleoside Scaffolds via Catalytic Cyclopropanation of 4-exo-Methylene Furanosides.

Jonas Verhoeven, L. Meerpoel, J. Thuring, 2021, The Journal of organic chemistry.

Synthesis of Cyclopropyl Pinacol Boronic Esters from Dibromocyclopropanes

Jonas Verhoeven, L. Meerpoel, J. Thuring, 2022, Synlett.

Preparation of Novel 4′-Spirocyclopropyl Nucleoside Analogues

V. Pande, Jonas Verhoeven, L. Meerpoel, 2021, Synlett.

Discovery of JNJ-63576253: A Clinical Stage Androgen Receptor Antagonist for F877L Mutant and Wild-Type Castration-Resistant Prostate Cancer (mCRPC).

Yolanda T. Chong, T. Bush, G. Bignan, 2021, Journal of medicinal chemistry.

Pd(0)-Catalyzed Direct Inter- and Intramolecular C–H Functionalization of 4-Carboxyimidazoles

L. Meerpoel, P. Angibaud, C. Hoarau, 2020, Synlett.

Chemoselective Palladium‐Catalyzed Direct C–H Arylation of 5‐Carboxyimidazoles: Unparalleled Access to Fused Imidazole‐Based Tricycles Containing Six‐, Seven‐ or Eight‐Membered Rings

L. Meerpoel, P. Angibaud, C. Hoarau, 2017 .

Structure-Based Design of Type II Inhibitors Applied to Maternal Embryonic Leucine Zipper Kinase.

V. Berdini, D. Brehmer, J. Linders, 2015, ACS medicinal chemistry letters.

MELK-T1, a small-molecule inhibitor of protein kinase MELK, decreases DNA-damage tolerance in proliferating cancer cells

M. Bollen, D. Brehmer, M. Paradé, 2015, Bioscience reports.

Liquid chromatography-mass spectrometry with chemiluminescent nitrogen detection for on-line quantitative analysis of compound collections: advantages and limitations.

L. Meerpoel, D. Corens, M. Schroven, 2004, Journal of chromatography. A.

Triphenylphosphine: A Catalyst for the Synthesis of C‐Aryl Furanosides from Furanosyl Halides.

I. Stansfield, L. Meerpoel, J. Cossy, 2014 .

Discovery and optimization of a series of small-molecule allosteric inhibitors of MALT1 protease.

J. Edwards, Tianbao Lu, U. Philippar, 2019, Bioorganic & medicinal chemistry letters.

Tandem Suzuki-Miyaura coupling/acid-catalyzed cyclization between vinyl ether boronates and vinyl halides: a concise approach to polysubstituted furans.

I. Stansfield, L. Meerpoel, J. Cossy, 2013, Organic letters.

Ruthenium-Catalyzed Reductive Arylation of N-(2-Pyridinyl)amides with Isopropanol and Arylboronate Esters.

Thomas O. Ronson, B. Maes, L. Meerpoel, 2018, Angewandte Chemie.

Abstract 4747: Design and synthesis of a series highly potent and bioavailable FASN KR domain inhibitors for cancer

Tianbao Lu, G. Bignan, M. Cummings, 2014 .

Synthesis and in vitro and in vivo Antifungal Activity of the Hydroxy Metabolites of Saperconazole

J. Heeres, M. Oris, L. Meerpoel, 2010, ChemMedChem.