List of works - Marc Le Borgne

1D NMR WaterLOGSY as an efficient method for fragment-based lead discovery

scientific article published on 01 December 2019

1H and 13C NMR assignments of bioactive indeno[1,2-b]indole-10-one derivatives.

scientific article

1st Joint European Conference on Therapeutic Targets and Medicinal Chemistry (TTMC 2015)

scientific article

2- and 3-[(aryl)(azolyl)methyl]indoles as potential non-steroidal aromatase inhibitors.

scientific article published in December 2004

2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 1. Identification of an Allosteric Binding Site

scientific article published on 18 February 2019

2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 2. Structure-Based Optimization and Investigation of Effects Specific to the Allosteric Mode of Action

scientific article published on 13 February 2019

2-Indolylmethylenebenzofuranones as first effective inhibitors of ABCC2.

scientific article

4,5,7-Trisubstituted indeno[1,2-b]indole inhibits CK2 activity in tumor cells equivalent to CX-4945 and shows strong anti-migratory effects

scientific article published on 18 December 2021

A 3D-QSAR CoMSIA study on 3-azolylmethylindoles as anti-leishmanial agents

scientific article

A safe and practical method for the preparation of 7α-thioether and thioester derivatives of spironolactone

scientific article

An Updated View on an Emerging Target: Selected Papers from the 8th International Conference on Protein Kinase CK2.

scientific article published on 23 March 2017

Antileishmanial activities and mechanisms of action of indole-based azoles

scientific article published on 01 June 2006

Biological exploration of a novel 1,2,4-triazole-indole hybrid molecule as antifungal agent

scientific article published on 01 December 2020

Biologically active carbazole derivatives: focus on oxazinocarbazoles and related compounds.

scientific article published on 3 April 2014

Biomimetic synthesis of Tramadol

scientific article published in 2015

Carbazole scaffolds in cancer therapy: a review from 2012 to 2018

scientific article published on 01 December 2019

Converting potent indeno[1,2-b]indole inhibitors of protein kinase CK2 into selective inhibitors of the breast cancer resistance protein ABCG2.

scientific article published on 16 October 2014

Crystal structure of 13-phenyl-2,3,4,13-tetra-hydro-1H-indazolo[1,2-b]phthalazine-1,6,11-trione

scientific article published on 12 December 2015

Design of new antifungal agents: synthesis and evaluation of 1-[(1H-indol-5-ylmethyl)amino]-2-phenyl-3-(1H-1,2,4-triazol-1-yl)propan-2-ols.

scientific article published on 31 August 2009

Design, synthesis and evaluation of 3-(imidazol- 1-ylmethyl)indoles as antileishmanial agents. Part II.

scientific article published in October 2009

Design, synthesis, and evaluation of 1-(N-benzylamino)-2-phenyl-3-(1H-1,2,4-triazol-1-yl)propan-2-ols as antifungal agents

scientific article published on 14 February 2008

Design, synthesis, and in vitro antifungal activity of 1-[(4-substituted-benzyl)methylamino]-2-(2,4-difluorophenyl)-3-(1H-1,2,4-triazol-1-yl)propan-2-ols

scientific article

Development of Pharmacophore Model for Indeno[1,2-b]indoles as Human Protein Kinase CK2 Inhibitors and Database Mining

scientific article published on 9 January 2017

Diacritic Binding of an Indenoindole Inhibitor by CK2α Paralogs Explored by a Reliable Path to Atomic Resolution CK2α' Structures

scientific article published on 19 March 2019

Discovery of (7-aryl-1,5-naphthyridin-2-yl)ureas as dual inhibitors of ERK2 and Aurora B kinases with antiproliferative activity against cancer cells.

scientific article

Discovery of 7-aryl-substituted (1,5-naphthyridin-4-yl)ureas as aurora kinase inhibitors.

scientific article published on 24 November 2013

Discovery of holoenzyme-disrupting chemicals as substrate-selective CK2 inhibitors

scientific article published on 04 November 2019

Enhancement of iodinin solubility by encapsulation into cyclodextrin nanoparticles.

scientific article published in December 2018

Functional display of heterotetrameric human protein kinase CK2 on Escherichia coli: a novel tool for drug discovery

scientific article

Improved Surface Display of Human Hyal1 and Identification of Testosterone Propionate and Chicoric Acid as New Inhibitors

scientific article published on 26 March 2020

In Search of Small Molecule Inhibitors Targeting the Flexible CK2 Subunit Interface

scientific article published on 03 February 2017

In vitro activity of a new antifungal azolyl-substituted indole against Aspergillus fumigatus

scientific article published in December 2002

In vitro modulation of multidrug resistance by pregnane steroids and in vivo inhibition of tumour development by 7α-OBz-11α(R)-OTHP-5β-pregnanedione in K562/R7 and H295R cell xenografts

article

Indeno[1,2-b]indole derivatives as a novel class of potent human protein kinase CK2 inhibitors.

scientific article

Indenoindoles and cyclopentacarbazoles as bioactive compounds: synthesis and biological applications.

scientific article published on 16 September 2013

Inhibition of Shiga toxin-converting bacteriophage development by novel antioxidant compounds.

scientific article published in December 2018

Mechanisms of depolymerization and activation of a polysialic acid and its tetramer by hydrogen peroxide

scientific article published on 21 September 2014

Mechanistic basis of breast cancer resistance protein inhibition by new indeno[1,2-b]indoles

scientific article published on 19 January 2021

New selective nonsteroidal aromatase inhibitors: synthesis and inhibitory activity of 2,3 or 5-(alpha-azolylbenzyl)-1H-indoles

scientific article published on 01 February 1999

Ninhydrins inhibit carbonic anhydrases directly binding to the metal ion

scientific article published on 05 October 2020

Occurrence of the synthetic analgesic tramadol in an African medicinal plant

scientific article

Oxidation of sialic acid using hydrogen peroxide as a new method to tune the reducing activity

scientific article published on 14 January 2014

Phenolic indeno[1,2-b]indoles as ABCG2-selective potent and non-toxic inhibitors stimulating basal ATPase activity

scientific article published on 3 July 2015

Potential application of plant lipid transfer proteins for drug delivery.

scientific article

Preparation and characterization of CK2 inhibitor-loaded cyclodextrin nanoparticles for drug delivery

scientific article published on 13 November 2012

Preparation and pharmacological profile of 7-(alpha-azolylbenzyl)-1H-indoles and indolines as new aromatase inhibitors

scientific article published in May 2003

Proceedings of the 16th annual conference of the Groupement des Pharmacochimistes de l'Arc Atlantique (GP2A)

scientific article published on 01 October 2008

QSAR Model of Indeno[1,2-b]indole Derivatives and Identification of N-isopentyl-2-methyl-4,9-dioxo-4,9-Dihydronaphtho[2,3-b]furan-3-carboxamide as a Potent CK2 Inhibitor

scientific article published on 26 December 2019

Screening of indeno[1,2-b]indoloquinones by MALDI-MS: a new set of potential CDC25 phosphatase inhibitors brought to light

scientific article

Self-Assembled Supramolecular Nanoparticles Improve the Cytotoxic Efficacy of CK2 Inhibitor THN7.

scientific article

Sleep Disorders and Therapeutic Management: A Survey in a French Population of Prisoners.

scientific article published on January 2017

Solubility enhancement of mefenamic acid by inclusion complex with β-cyclodextrin: <i>in silico</i> modelling, formulation, characterisation, and <i>in vitro</i> studies

scientific article published on 01 December 2021

Structural elucidation of two photolytic degradation products of tetrabenazine

scientific article published on 03 January 2014

Structure-based design and profiling of novel 17β-HSD14 inhibitors

scientific article published on 22 May 2018

Synthesis and Preclinical Evaluation of TPA-Based Zinc Chelators as Metallo-β-lactamase Inhibitors

scientific article published on 02 August 2018

Synthesis and antifungal activities of new fluconazole analogues with azaheterocycle moiety

scientific article published on 19 April 2007

Synthesis and antifungal activity of new 1-halogenobenzyl-3-imidazolylmethylindole derivatives

scientific article published in January 2003

Synthesis and antileishmanial activity of 3-(alpha-azolylbenzyl)indoles

scientific article published in December 2002

Synthesis and biological evaluation of 3-(azolylmethyl)-1H-indoles and 3-(alpha-azolylbenzyl)-1H-indoles as selective aromatase inhibitors

scientific article published in October 2007

Synthesis and biological evaluation of 5-[(aryl)(1H-imidazol-1-yl)methyl]-1H-indoles: potent and selective aromatase inhibitors

scientific article published on 27 December 2005

Synthesis and biological evaluation of novel substituted pyrrolo[1,2-a]quinoxaline derivatives as inhibitors of the human protein kinase CK2.

scientific article published on 3 May 2013

Synthesis and biological evaluation of zinc chelating compounds as metallo-β-lactamase inhibitors

scientific article published on 08 March 2019

Synthesis and in vitro evaluation of 3-(1-azolylmethyl)-1H-indoles and 3-(1-azolyl-1-phenylmethyl)-1H-indoles as inhibitors of P450 arom

scientific article published on 01 May 1997

Synthesis and structure-activity relationships of 2-phenyl-1-[(pyridinyl- and piperidinylmethyl)amino]-3-(1H-1,2,4-triazol-1-yl)propan-2-ols as antifungal agents.

scientific article published on 3 December 2008

Synthesis of 6- or 4-functionalized indoles via a reductive cyclization approach and evaluation as aromatase inhibitors

scientific article published on 3 July 2008

Synthesis of new steroidal inhibitors of P-glycoprotein-mediated multidrug resistance and biological evaluation on K562/R7 erythroleukemia cells

scientific article published on 11 February 2015

Synthesis, Optimization, Antifungal Activity, Selectivity, and CYP51 Binding of New 2-Aryl-3-azolyl-1-indolyl-propan-2-ols

scientific article published on 08 August 2020

Synthesis, Spectroscopic Characterization, and In Vitro Antibacterial Evaluation of Novel Functionalized Sulfamidocarbonyloxyphosphonates

scientific article published on 10 July 2018

Synthesis, X-ray structure, in silico calculation, and carbonic anhydrase inhibitory properties of benzylimidazole metal complexes

scientific article published on 01 December 2018

Three-dimensional model of cytochrome P450 human aromatase.

scientific article published in December 2005

Toward selective CK2alpha and CK2alpha' inhibitors: Development of a novel whole-cell kinase assay by Autodisplay of catalytic CK2alpha'.

scientific article published on 8 January 2016

Toxicological Risks of the Cobalt–Chromium Alloys in Dentistry: A Systematic Review

scientific article published in 2022

Uncompetitive nanomolar dimeric indenoindole inhibitors of the human breast cancer resistance pump ABCG2

scientific article published on 12 November 2020

Unexpected Binding Mode of a Potent Indeno[1,2-b]indole-Type Inhibitor of Protein Kinase CK2 Revealed by Complex Structures with the Catalytic Subunit CK2α and Its Paralog CK2α'.

scientific article published on 13 December 2017

[Synthesis and biological evaluation of indole derivatives acting as anti-inflammatory or antitumoral drugs]

scientific article published on 01 October 2000

List of works by Marc Le Borgne

1D NMR WaterLOGSY as an efficient method for fragment-based lead discovery

1H and 13C NMR assignments of bioactive indeno[1,2-b]indole-10-one derivatives.

1st Joint European Conference on Therapeutic Targets and Medicinal Chemistry (TTMC 2015)

2- and 3-[(aryl)(azolyl)methyl]indoles as potential non-steroidal aromatase inhibitors.

2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 1. Identification of an Allosteric Binding Site

2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 2. Structure-Based Optimization and Investigation of Effects Specific to the Allosteric Mode of Action

2-Indolylmethylenebenzofuranones as first effective inhibitors of ABCC2.

4,5,7-Trisubstituted indeno[1,2-b]indole inhibits CK2 activity in tumor cells equivalent to CX-4945 and shows strong anti-migratory effects

A 3D-QSAR CoMSIA study on 3-azolylmethylindoles as anti-leishmanial agents

A safe and practical method for the preparation of 7α-thioether and thioester derivatives of spironolactone

An Updated View on an Emerging Target: Selected Papers from the 8th International Conference on Protein Kinase CK2.

Antileishmanial activities and mechanisms of action of indole-based azoles

Biological exploration of a novel 1,2,4-triazole-indole hybrid molecule as antifungal agent

Biologically active carbazole derivatives: focus on oxazinocarbazoles and related compounds.

Biomimetic synthesis of Tramadol

Carbazole scaffolds in cancer therapy: a review from 2012 to 2018

Converting potent indeno[1,2-b]indole inhibitors of protein kinase CK2 into selective inhibitors of the breast cancer resistance protein ABCG2.

Crystal structure of 13-phenyl-2,3,4,13-tetra-hydro-1H-indazolo[1,2-b]phthalazine-1,6,11-trione

Design of new antifungal agents: synthesis and evaluation of 1-[(1H-indol-5-ylmethyl)amino]-2-phenyl-3-(1H-1,2,4-triazol-1-yl)propan-2-ols.

Design, synthesis and evaluation of 3-(imidazol- 1-ylmethyl)indoles as antileishmanial agents. Part II.

Design, synthesis, and evaluation of 1-(N-benzylamino)-2-phenyl-3-(1H-1,2,4-triazol-1-yl)propan-2-ols as antifungal agents

Design, synthesis, and in vitro antifungal activity of 1-[(4-substituted-benzyl)methylamino]-2-(2,4-difluorophenyl)-3-(1H-1,2,4-triazol-1-yl)propan-2-ols

Development of Pharmacophore Model for Indeno[1,2-b]indoles as Human Protein Kinase CK2 Inhibitors and Database Mining

Diacritic Binding of an Indenoindole Inhibitor by CK2α Paralogs Explored by a Reliable Path to Atomic Resolution CK2α' Structures

Discovery of (7-aryl-1,5-naphthyridin-2-yl)ureas as dual inhibitors of ERK2 and Aurora B kinases with antiproliferative activity against cancer cells.

Discovery of 7-aryl-substituted (1,5-naphthyridin-4-yl)ureas as aurora kinase inhibitors.

Discovery of holoenzyme-disrupting chemicals as substrate-selective CK2 inhibitors

Enhancement of iodinin solubility by encapsulation into cyclodextrin nanoparticles.

Functional display of heterotetrameric human protein kinase CK2 on Escherichia coli: a novel tool for drug discovery

Improved Surface Display of Human Hyal1 and Identification of Testosterone Propionate and Chicoric Acid as New Inhibitors

In Search of Small Molecule Inhibitors Targeting the Flexible CK2 Subunit Interface

In vitro activity of a new antifungal azolyl-substituted indole against Aspergillus fumigatus

In vitro modulation of multidrug resistance by pregnane steroids and in vivo inhibition of tumour development by 7α-OBz-11α(R)-OTHP-5β-pregnanedione in K562/R7 and H295R cell xenografts

Indeno[1,2-b]indole derivatives as a novel class of potent human protein kinase CK2 inhibitors.

Indenoindoles and cyclopentacarbazoles as bioactive compounds: synthesis and biological applications.

Inhibition of Shiga toxin-converting bacteriophage development by novel antioxidant compounds.

Mechanisms of depolymerization and activation of a polysialic acid and its tetramer by hydrogen peroxide

Mechanistic basis of breast cancer resistance protein inhibition by new indeno[1,2-b]indoles

New selective nonsteroidal aromatase inhibitors: synthesis and inhibitory activity of 2,3 or 5-(alpha-azolylbenzyl)-1H-indoles

Ninhydrins inhibit carbonic anhydrases directly binding to the metal ion

Occurrence of the synthetic analgesic tramadol in an African medicinal plant

Oxidation of sialic acid using hydrogen peroxide as a new method to tune the reducing activity

Phenolic indeno[1,2-b]indoles as ABCG2-selective potent and non-toxic inhibitors stimulating basal ATPase activity

Potential application of plant lipid transfer proteins for drug delivery.

Preparation and characterization of CK2 inhibitor-loaded cyclodextrin nanoparticles for drug delivery

Preparation and pharmacological profile of 7-(alpha-azolylbenzyl)-1H-indoles and indolines as new aromatase inhibitors

Proceedings of the 16th annual conference of the Groupement des Pharmacochimistes de l'Arc Atlantique (GP2A)

QSAR Model of Indeno[1,2-b]indole Derivatives and Identification of N-isopentyl-2-methyl-4,9-dioxo-4,9-Dihydronaphtho[2,3-b]furan-3-carboxamide as a Potent CK2 Inhibitor

Screening of indeno[1,2-b]indoloquinones by MALDI-MS: a new set of potential CDC25 phosphatase inhibitors brought to light

Self-Assembled Supramolecular Nanoparticles Improve the Cytotoxic Efficacy of CK2 Inhibitor THN7.

Sleep Disorders and Therapeutic Management: A Survey in a French Population of Prisoners.

Solubility enhancement of mefenamic acid by inclusion complex with β-cyclodextrin: <i>in silico</i> modelling, formulation, characterisation, and <i>in vitro</i> studies

Structural elucidation of two photolytic degradation products of tetrabenazine

Structure-based design and profiling of novel 17β-HSD14 inhibitors

Synthesis and Preclinical Evaluation of TPA-Based Zinc Chelators as Metallo-β-lactamase Inhibitors

Synthesis and antifungal activities of new fluconazole analogues with azaheterocycle moiety

Synthesis and antifungal activity of new 1-halogenobenzyl-3-imidazolylmethylindole derivatives

Synthesis and antileishmanial activity of 3-(alpha-azolylbenzyl)indoles

Synthesis and biological evaluation of 3-(azolylmethyl)-1H-indoles and 3-(alpha-azolylbenzyl)-1H-indoles as selective aromatase inhibitors

Synthesis and biological evaluation of 5-[(aryl)(1H-imidazol-1-yl)methyl]-1H-indoles: potent and selective aromatase inhibitors

Synthesis and biological evaluation of novel substituted pyrrolo[1,2-a]quinoxaline derivatives as inhibitors of the human protein kinase CK2.

Synthesis and biological evaluation of zinc chelating compounds as metallo-β-lactamase inhibitors

Synthesis and in vitro evaluation of 3-(1-azolylmethyl)-1H-indoles and 3-(1-azolyl-1-phenylmethyl)-1H-indoles as inhibitors of P450 arom

Synthesis and structure-activity relationships of 2-phenyl-1-[(pyridinyl- and piperidinylmethyl)amino]-3-(1H-1,2,4-triazol-1-yl)propan-2-ols as antifungal agents.

Synthesis of 6- or 4-functionalized indoles via a reductive cyclization approach and evaluation as aromatase inhibitors

Synthesis of new steroidal inhibitors of P-glycoprotein-mediated multidrug resistance and biological evaluation on K562/R7 erythroleukemia cells

Synthesis, Optimization, Antifungal Activity, Selectivity, and CYP51 Binding of New 2-Aryl-3-azolyl-1-indolyl-propan-2-ols

Synthesis, Spectroscopic Characterization, and In Vitro Antibacterial Evaluation of Novel Functionalized Sulfamidocarbonyloxyphosphonates

Synthesis, X-ray structure, in silico calculation, and carbonic anhydrase inhibitory properties of benzylimidazole metal complexes

Three-dimensional model of cytochrome P450 human aromatase.

Toward selective CK2alpha and CK2alpha' inhibitors: Development of a novel whole-cell kinase assay by Autodisplay of catalytic CK2alpha'.

Toxicological Risks of the Cobalt–Chromium Alloys in Dentistry: A Systematic Review

Uncompetitive nanomolar dimeric indenoindole inhibitors of the human breast cancer resistance pump ABCG2

Unexpected Binding Mode of a Potent Indeno[1,2-b]indole-Type Inhibitor of Protein Kinase CK2 Revealed by Complex Structures with the Catalytic Subunit CK2α and Its Paralog CK2α'.

[Synthesis and biological evaluation of indole derivatives acting as anti-inflammatory or antitumoral drugs]