List of works - Steven De Jonghe

A Scaffold-Hopping Strategy toward the Identification of Inhibitors of Cyclin G Associated Kinase

scientific article published on 02 January 2019

A Set of Experimentally Validated Decoys for the Human CC Chemokine Receptor 7 (CCR7) Obtained by Virtual Screening

scientific article published on 18 March 2022

A new alkaloid from Pancratium maritimum - Structure elucidation using computer-assisted structure elucidation (CASE) and evaluation of cytotoxicity and anti-SARS-CoV-2 activity

scientific article published in December 2023

A short and straightforward approach towards 6-amino and 6-aminoalkyl thiazolo[4,5-c]pyridazines

Amidate Prodrugs of Cyclic 9-()-[3-Hydroxy-2-(phosphonomethoxy)propyl]adenine with Potent Anti-Herpesvirus Activity

Amidate Prodrugs of Deoxythreosyl Nucleoside Phosphonates as Dual Inhibitors of HIV and HBV Replication

scientific article published on 17 October 2016

Anticancer kinase inhibitors impair intracellular viral trafficking and exert broad-spectrum antiviral effects

scientific article published on 27 February 2017

Aspartic acid based nucleoside phosphoramidate prodrugs as potent inhibitors of hepatitis C virus replication

scientific article published on May 2015

Astemizole analogues with reduced hERG inhibition as potent antimalarial compounds.

scientific article published on 7 October 2017

Bicyclic α-Iminophosphonates as High Affinity Imidazoline I2 Receptor Ligands for Alzheimer's Disease

scientific article published on 19 March 2020

Bifunctional aryloxyphosphoramidate prodrugs of 2'-C-Me-uridine: synthesis and anti-HCV activity

scientific article published on September 2016

Biopharmaceutical profiling of a pyrido[4,3-d] pyrimidine compound library ⬇️

scientific article published on August 7, 2013

Correction to Bicyclic α-Iminophosphonates as High Affinity Imidazoline I2 Receptor Ligands for Alzheimer's Disease

scientific article published on 14 September 2020

Cyclin G-associated kinase (GAK) affinity and antiviral activity studies of a series of 3-C-substituted isothiazolo[4,3-b]pyridines

scientific article published on 28 November 2018

Design, synthesis and biological evaluation of pyrazolo[3,4-d]pyrimidine-based protein kinase D inhibitors

scientific article published on 29 July 2020

Development of Synthetic Strategies for the Construction of Pyrido[4,3-d]pyrimidine Libraries – the Discovery of a New Class of PDE-4 Inhibitors

article

Development of Synthetic Strategies for the Construction of Pyrido[4,3-d]pyrimidine Libraries — The Discovery of a New Class of PDE-4 Inhibitors

Discovery of 7-N-Piperazinylthiazolo[5,4-d]pyrimidine Analogues as a Novel Class of Immunosuppressive Agents with in Vivo Biological Activity

Discovery of a new Mycobacterium tuberculosis thymidylate synthase X inhibitor with a unique inhibition profile

scientific article published on 27 March 2017

Discovery of an acyclic nucleoside phosphonate that inhibits Mycobacterium tuberculosis ThyX based on the binding mode of a 5-alkynyl substrate analogue

scientific article

Discovery of dual death-associated protein related apoptosis inducing protein kinase 1 and 2 inhibitors by a scaffold hopping approach

scientific article

Emimycin and its nucleoside derivatives: Synthesis and antiviral activity

scientific article published on 7 December 2017

Expanding the Antiviral Spectrum of 3-Fluoro-2-(phosphonomethoxy)propyl Acyclic Nucleoside Phosphonates: Diamyl Aspartate Amidate Prodrugs

scientific article published on 6 July 2017

Gelatin degradation assay reveals MMP-9 inhibitors and function of O-glycosylated domain

scientific article

Identification and evaluation of potential SARS-CoV-2 antiviral agents targeting mRNA cap guanine N7-Methyltransferase

scientific article

Imidazopyridine- and purine-thioacetamide derivatives: potent inhibitors of nucleotide pyrophosphatase/phosphodiesterase 1 (NPP1).

scientific article

In vitro disposition profiling of heterocyclic compounds

scientific article published on June 2015

Isothiazolo[4,3-b]pyridines as inhibitors of cyclin G associated kinase : synthesis, structure-activity relationship studies and antiviral activity.

scientific article published on 07 August 2015

L-Aspartic and l-glutamic acid ester-based ProTides of anticancer nucleosides: Synthesis and antitumoral evaluation

scientific article published on 22 March 2016

Optimization of Isothiazolo[4,3- b]pyridine-Based Inhibitors of Cyclin G Associated Kinase (GAK) with Broad-Spectrum Antiviral Activity

scientific article published on 16 July 2018

Regioselective cross-coupling reactions and nucleophilic aromatic substitutions on a 5,7-dichloropyrido[4,3-d]pyrimidine scaffold

Scalable Synthesis, In Vitro cccDNA Reduction, and In Vivo Antihepatitis B Virus Activity of a Phosphonomethoxydeoxythreosyl Adenine Prodrug

scientific article published on 16 November 2020

Selective Inhibitors of Cyclin G Associated Kinase (GAK) as Anti-Hepatitis C Agents

scientific article

Sliding of HIV-1 reverse transcriptase over DNA creates a transient P pocket - targeting P-pocket by fragment screening

scientific article published on 08 December 2021

Stimulation of the atypical chemokine receptor 3 (ACKR3) by a small-molecule agonist attenuates fibrosis in a preclinical liver but not lung injury model

scientific article published on 13 May 2022

Structure-activity relationship study of the pyridine moiety of isothiazolo[4,3-b]pyridines as antiviral agents targeting cyclin G-associated kinase

scientific article published on 11 November 2019

Substrate-Dependence of Competitive Nucleotide Pyrophosphatase/Phosphodiesterase1 (NPP1) Inhibitors

scientific article published on 15 February 2017

Synthesis and Biological Evaluation of Pyrrolo[2,1-f][1,2,4]triazine C-Nucleosides with a Ribose, 2'-Deoxyribose, and 2',3'-Dideoxyribose Sugar Moiety

scientific article published on 21 November 2017

Synthesis and Structure-Activity Relationship Studies of Benzo[b][1,4]oxazin-3(4H)-one Analogues as Inhibitors of Mycobacterial Thymidylate Synthase X

scientific article published on 20 February 2019

Synthesis and anti-HIV activity of guanine modified fluorinated acyclic nucleoside phosphonates derivatives

article

Synthesis and antibacterial evaluation of a novel series of 2-(1,2-dihydro-3-oxo-3H-pyrazol-2-yl)benzothiazoles

scientific article

Synthesis and antiviral evaluation of base-modified deoxythreosyl nucleoside phosphonates

scientific article published on 19 June 2017

Synthesis and antiviral evaluation of cyclopentyl nucleoside phosphonates.

scientific article

Synthesis and cancer cell cytotoxicity of 2-heteroaryl-4-(4-heteroaryl-2-oxobut-3-en-1-ylidene)-substituted benzothiazepanes

scholarly article

Synthesis and cytotoxic evaluation of monocarbonyl curcuminoids and their pyrazoline derivatives

scientific article published in 2019

Synthesis and evaluation of 5-substituted 2'-deoxyuridine monophosphate analogues as inhibitors of flavin-dependent thymidylate synthase in Mycobacterium tuberculosis

scientific article published on 9 June 2011

Synthesis and evaluation of 6-aza-2'-deoxyuridine monophosphate analogs as inhibitors of thymidylate synthases, and as substrates or inhibitors of thymidine monophosphate kinase in Mycobacterium tuberculosis.

scientific article

Synthesis and evaluation of novel ligands for the histamine H₄ receptor based on a pyrrolo[2,3-d]pyrimidine scaffold

scientific article published on 15 November 2012

Synthesis and in vitro evaluation of 2-amino-4-N-piperazinyl-6-(3,4-dimethoxyphenyl)-pteridines as dual immunosuppressive and anti-inflammatory agents

scientific article published on 16 November 2010

Synthesis and structure-activity relationship studies of 2-(1,3,4-oxadiazole-2(3H)-thione)-3-amino-5-arylthieno[2,3-b]pyridines as inhibitors of DRAK2.

scientific article

Synthesis and structure-activity relationships of 3,5-disubstituted-pyrrolo[2,3- b]pyridines as inhibitors of adaptor associated kinase 1 (AAK1) with antiviral activity

scientific article published on 12 June 2019

Synthesis of 6-aryl-2′-deoxyuridine nucleosides via a Liebeskind cross-coupling methodology

Synthesis of Novel Nitroxoline Analogs with Potent Cathepsin B Exopeptidase Inhibitory Activity

scientific article published on 03 August 2020

Synthesis of Protected Amino Hexitol Nucleosides as Building Blocks for Oligonucleotide Synthesis

scientific article published on 07 December 2018

Synthesis of a 2,4,6-trisubstituted 5-cyano-pyrimidine library and evaluation of its immunosuppressive activity in a Mixed Lymphocyte Reaction assay

scientific article

Synthesis of a 3'-Fluoro-3'-deoxytetrose Adenine Phosphonate.

scientific article

Synthesis of a C-Nucleoside Phosphonate by Base-Promoted Epimerization

scientific article published on 01 February 2018

Synthesis of a Nucleobase-Modified ProTide Library

scientific article

Synthesis of homoceramides, novel ceramide analogues, and their lack of effect on the growth of hippocampal neurons

scientific article published in February 2002

Synthesis of novel 5-amino-thiazolo[4,5-d]pyrimidines as E. coli and S. aureus SecA inhibitors

scientific article

Synthesis, immunosuppressive activity and structure-activity relationship study of a new series of 4-N-piperazinyl-thieno[2,3-d]pyrimidine analogues

scientific article published on 4 January 2010

Tenofovir-Amino Acid Conjugates Act as Polymerase Substrates-Implications for Avoiding Cellular Phosphorylation in the Discovery of Nucleotide Analogues

scientific article published on 23 December 2020

Thiazolo[3,2-a]benzimidazol-3(2H)-one derivatives: Structure-activity relationships of selective nucleotide pyrophosphatase/phosphodiesterase1 (NPP1) inhibitors

scientific article published on 21 May 2016

Ultralarge Virtual Screening Identifies SARS-CoV-2 Main Protease Inhibitors with Broad-Spectrum Activity against Coronaviruses

scientific article published on 10 February 2022

List of works by Steven De Jonghe

A Scaffold-Hopping Strategy toward the Identification of Inhibitors of Cyclin G Associated Kinase

A Set of Experimentally Validated Decoys for the Human CC Chemokine Receptor 7 (CCR7) Obtained by Virtual Screening

A new alkaloid from Pancratium maritimum - Structure elucidation using computer-assisted structure elucidation (CASE) and evaluation of cytotoxicity and anti-SARS-CoV-2 activity

A short and straightforward approach towards 6-amino and 6-aminoalkyl thiazolo[4,5-c]pyridazines

Amidate Prodrugs of Cyclic 9-()-[3-Hydroxy-2-(phosphonomethoxy)propyl]adenine with Potent Anti-Herpesvirus Activity

Amidate Prodrugs of Deoxythreosyl Nucleoside Phosphonates as Dual Inhibitors of HIV and HBV Replication

Anticancer kinase inhibitors impair intracellular viral trafficking and exert broad-spectrum antiviral effects

Aspartic acid based nucleoside phosphoramidate prodrugs as potent inhibitors of hepatitis C virus replication

Astemizole analogues with reduced hERG inhibition as potent antimalarial compounds.

Bicyclic α-Iminophosphonates as High Affinity Imidazoline I2 Receptor Ligands for Alzheimer's Disease

Bifunctional aryloxyphosphoramidate prodrugs of 2'-C-Me-uridine: synthesis and anti-HCV activity

Biopharmaceutical profiling of a pyrido[4,3-d] pyrimidine compound library ⬇️

Correction to Bicyclic α-Iminophosphonates as High Affinity Imidazoline I2 Receptor Ligands for Alzheimer's Disease

Cyclin G-associated kinase (GAK) affinity and antiviral activity studies of a series of 3-C-substituted isothiazolo[4,3-b]pyridines

Design, synthesis and biological evaluation of pyrazolo[3,4-d]pyrimidine-based protein kinase D inhibitors

Development of Synthetic Strategies for the Construction of Pyrido[4,3-d]pyrimidine Libraries – the Discovery of a New Class of PDE-4 Inhibitors

Development of Synthetic Strategies for the Construction of Pyrido[4,3-d]pyrimidine Libraries — The Discovery of a New Class of PDE-4 Inhibitors

Discovery of 7-N-Piperazinylthiazolo[5,4-d]pyrimidine Analogues as a Novel Class of Immunosuppressive Agents with in Vivo Biological Activity

Discovery of a new Mycobacterium tuberculosis thymidylate synthase X inhibitor with a unique inhibition profile

Discovery of an acyclic nucleoside phosphonate that inhibits Mycobacterium tuberculosis ThyX based on the binding mode of a 5-alkynyl substrate analogue

Discovery of dual death-associated protein related apoptosis inducing protein kinase 1 and 2 inhibitors by a scaffold hopping approach

Emimycin and its nucleoside derivatives: Synthesis and antiviral activity

Expanding the Antiviral Spectrum of 3-Fluoro-2-(phosphonomethoxy)propyl Acyclic Nucleoside Phosphonates: Diamyl Aspartate Amidate Prodrugs

Gelatin degradation assay reveals MMP-9 inhibitors and function of O-glycosylated domain

Identification and evaluation of potential SARS-CoV-2 antiviral agents targeting mRNA cap guanine N7-Methyltransferase

Imidazopyridine- and purine-thioacetamide derivatives: potent inhibitors of nucleotide pyrophosphatase/phosphodiesterase 1 (NPP1).

In vitro disposition profiling of heterocyclic compounds

Isothiazolo[4,3-b]pyridines as inhibitors of cyclin G associated kinase : synthesis, structure-activity relationship studies and antiviral activity.

L-Aspartic and l-glutamic acid ester-based ProTides of anticancer nucleosides: Synthesis and antitumoral evaluation

Optimization of Isothiazolo[4,3- b]pyridine-Based Inhibitors of Cyclin G Associated Kinase (GAK) with Broad-Spectrum Antiviral Activity

Regioselective cross-coupling reactions and nucleophilic aromatic substitutions on a 5,7-dichloropyrido[4,3-d]pyrimidine scaffold

Scalable Synthesis, In Vitro cccDNA Reduction, and In Vivo Antihepatitis B Virus Activity of a Phosphonomethoxydeoxythreosyl Adenine Prodrug

Selective Inhibitors of Cyclin G Associated Kinase (GAK) as Anti-Hepatitis C Agents

Sliding of HIV-1 reverse transcriptase over DNA creates a transient P pocket - targeting P-pocket by fragment screening

Stimulation of the atypical chemokine receptor 3 (ACKR3) by a small-molecule agonist attenuates fibrosis in a preclinical liver but not lung injury model

Structure-activity relationship study of the pyridine moiety of isothiazolo[4,3-b]pyridines as antiviral agents targeting cyclin G-associated kinase

Substrate-Dependence of Competitive Nucleotide Pyrophosphatase/Phosphodiesterase1 (NPP1) Inhibitors

Synthesis and Biological Evaluation of Pyrrolo[2,1-f][1,2,4]triazine C-Nucleosides with a Ribose, 2'-Deoxyribose, and 2',3'-Dideoxyribose Sugar Moiety

Synthesis and Structure-Activity Relationship Studies of Benzo[b][1,4]oxazin-3(4H)-one Analogues as Inhibitors of Mycobacterial Thymidylate Synthase X

Synthesis and anti-HIV activity of guanine modified fluorinated acyclic nucleoside phosphonates derivatives

Synthesis and antibacterial evaluation of a novel series of 2-(1,2-dihydro-3-oxo-3H-pyrazol-2-yl)benzothiazoles

Synthesis and antiviral evaluation of base-modified deoxythreosyl nucleoside phosphonates

Synthesis and antiviral evaluation of cyclopentyl nucleoside phosphonates.

Synthesis and cancer cell cytotoxicity of 2-heteroaryl-4-(4-heteroaryl-2-oxobut-3-en-1-ylidene)-substituted benzothiazepanes

Synthesis and cytotoxic evaluation of monocarbonyl curcuminoids and their pyrazoline derivatives

Synthesis and evaluation of 5-substituted 2'-deoxyuridine monophosphate analogues as inhibitors of flavin-dependent thymidylate synthase in Mycobacterium tuberculosis

Synthesis and evaluation of 6-aza-2'-deoxyuridine monophosphate analogs as inhibitors of thymidylate synthases, and as substrates or inhibitors of thymidine monophosphate kinase in Mycobacterium tuberculosis.

Synthesis and evaluation of novel ligands for the histamine H₄ receptor based on a pyrrolo[2,3-d]pyrimidine scaffold

Synthesis and in vitro evaluation of 2-amino-4-N-piperazinyl-6-(3,4-dimethoxyphenyl)-pteridines as dual immunosuppressive and anti-inflammatory agents

Synthesis and structure-activity relationship studies of 2-(1,3,4-oxadiazole-2(3H)-thione)-3-amino-5-arylthieno[2,3-b]pyridines as inhibitors of DRAK2.

Synthesis and structure-activity relationships of 3,5-disubstituted-pyrrolo[2,3- b]pyridines as inhibitors of adaptor associated kinase 1 (AAK1) with antiviral activity

Synthesis of 6-aryl-2′-deoxyuridine nucleosides via a Liebeskind cross-coupling methodology

Synthesis of Novel Nitroxoline Analogs with Potent Cathepsin B Exopeptidase Inhibitory Activity

Synthesis of Protected Amino Hexitol Nucleosides as Building Blocks for Oligonucleotide Synthesis

Synthesis of a 2,4,6-trisubstituted 5-cyano-pyrimidine library and evaluation of its immunosuppressive activity in a Mixed Lymphocyte Reaction assay

Synthesis of a 3'-Fluoro-3'-deoxytetrose Adenine Phosphonate.

Synthesis of a C-Nucleoside Phosphonate by Base-Promoted Epimerization

Synthesis of a Nucleobase-Modified ProTide Library

Synthesis of homoceramides, novel ceramide analogues, and their lack of effect on the growth of hippocampal neurons

Synthesis of novel 5-amino-thiazolo[4,5-d]pyrimidines as E. coli and S. aureus SecA inhibitors

Synthesis, immunosuppressive activity and structure-activity relationship study of a new series of 4-N-piperazinyl-thieno[2,3-d]pyrimidine analogues

Tenofovir-Amino Acid Conjugates Act as Polymerase Substrates-Implications for Avoiding Cellular Phosphorylation in the Discovery of Nucleotide Analogues

Thiazolo[3,2-a]benzimidazol-3(2H)-one derivatives: Structure-activity relationships of selective nucleotide pyrophosphatase/phosphodiesterase1 (NPP1) inhibitors

Ultralarge Virtual Screening Identifies SARS-CoV-2 Main Protease Inhibitors with Broad-Spectrum Activity against Coronaviruses