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Keywords

3-bfuran-4 ADMET 2-bindoles ABCG2 inhibitors A427 cells Synthesis Cytotoxicity Indeno1 Cancer Inhibitors Candida species 9-dione Medicinal chemistry CK2 Protein kinase CK2 2-bindole scaffold 2-bindole Drug discovery X-ray crystallography ABCG2
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105

Marc Le Borgne

Main dates:

2021-      Member of Researh Cancer Centre of Lyon (CRCL) - Small Molecules for Biological Targets (SMBT) Team

2011/20   Director of the Research Team EA 4446 B2MC, UCBL.

2016-      Manager of Master 2 Conception and Optimization of Health Products (Health Engineering)

2009-       Student Exchange Correspondent with Canada and USA, Faculty of Pharmacy, UCBL.

2008        Recruitment as Professor in Medicinal Chemistry, Faculty of Pharmacy - University Lyon 1 (UCBL).

2007        Habilitation in Medicinal Chemistry, national examination - Paris.

2005/08   Vice-Dean in charge of general affairs, logistics and international cooperation, Faculty of Pharmacy - Univ. Nantes.

2003       Accreditation to supervise research (HDR diploma) in Medicinal Chemistry. Title: “Taylor-made molecules as aromatase inhibitors and antifungal agents” - Univ. Nantes.

2000        Research assistant (1997-1999) and Assistant Professor (2000-2008) in the Laboratory of Medicinal Chemistry, Faculty of Pharmacy - Univ. Nantes.

                Lecturer within the framework of continuing education of Pharmacists - Association of Post University Higher Education in Pharmacy - Region Loire-Atlantique.

1998        Thesis award in physico-chemical sciences, awarded by the French Academy of Pharmacy.

1997        Pharmaco-chemistry Ph-D at the Univ. Nantes.

1994        PharmD at the Univ. Nantes.

1992        Practice of Pharmacy (POP) at the Welsh School of Pharmacy.

Research field:

Design, synthesis and structural optimization of functionalized small molecules as anticancer agents, efflux pump inhibitors and anti-infective agents.

Some scaffolds developed: indole, naphthyridine, indeno[1,2-b]indole.

Education experience:

Medicinal Chemistry (design, synthesis, optimization, SAR analysis, ADMET, therapeutic uses).

Drug Lifecycle and Industrial Property Rights at Univ. Lyon 1.

Journal articles95 documents

  • Abdeslem Bouzina, Malika Berredjem, Billel Belhani, Sofiane Bouacida, Christelle Marminon, et al.. Microwave-accelerated multicomponent synthesis and X-ray characterization of novel benzothiadiazinone dioxide derivatives, analogues of Monastrol. Research on Chemical Intermediates, Springer Verlag, 2021, ⟨10.1007/s11164-020-04378-3⟩. ⟨hal-03112770⟩
  • Samer Haidar, Christelle Marminon, Dagmar Aichele, Abdelhamid Nacereddine, Wael Zeinyeh, et al.. 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. Molecules, MDPI, 2020, 25 (1), pp.97. ⟨10.3390/molecules25010097⟩. ⟨hal-02424862⟩
  • Fabrice Pagniez, Nicolas Lebouvier, Young Min Na, Isabelle Ourliac-Garnier, Carine Picot, et al.. Biological exploration of a novel 1,2,4-triazole-indole hybrid molecule as antifungal agent. Journal of Enzyme Inhibition and Medicinal Chemistry, Informa Healthcare, 2020, 35 (1), pp.398-403. ⟨10.1080/14756366.2019.1705292⟩. ⟨hal-02455791⟩
  • Abdeslem Bouzina, Malika Berredjem, Alessio Nocentini, Silvia Bua, Zouhair Bouaziz, et al.. Ninhydrins inhibit carbonic anhydrases directly binding to the metal ion. European Journal of Medicinal Chemistry, Elsevier, 2020, pp.112875. ⟨10.1016/j.ejmech.2020.112875⟩. ⟨hal-02963341⟩
  • Jean Guillon, Shweta Nim, Stéphane Moreau, Luisa Ronga, Solène Savrimoutou, et al.. Synthesis of new piperazinyl-pyrrolo[1,2- a ]quinoxaline derivatives as inhibitors of Candida albicans multidrug transporters by a Buchwald–Hartwig cross-coupling reaction. RSC Advances, Royal Society of Chemistry, 2020, 10 (5), pp.2915-2931. ⟨10.1039/C9RA09348F⟩. ⟨hal-02449065⟩
  • Nicolas Lebouvier, Fabrice Pagniez, Young Na, Da Shi, Patricia Pinson, et al.. Synthesis, Optimization, Antifungal Activity, Selectivity, and CYP51 Binding of New 2-Aryl-3-azolyl-1-indolyl-propan-2-ols. Pharmaceuticals, MDPI, 2020, 13 (8), 186 (32 p.). ⟨10.3390/ph13080186⟩. ⟨hal-02913479⟩
  • Alexandre Bancet, Claire Raingeval, Thierry Lomberget, Marc Le Borgne, Jean-François Guichou, et al.. No title. Journal of Medicinal Chemistry, American Chemical Society, 2020, 63 (20), pp.11420-11435. ⟨10.1021/acs.jmedchem.0c00242⟩. ⟨hal-02909120⟩
  • Alina Vaicelyte, Christine Janssen, Marc Le Borgne, Brigitte Grosgogeat. Cobalt–Chromium Dental Alloys: Metal Exposures, Toxicological Risks, CMR Classification, and EU Regulatory Framework. Crystals, MDPI, 2020, 10 (12), pp.1151. ⟨10.3390/cryst10121151⟩. ⟨hal-03088443⟩
  • Nathalie Guragossian, Billel Belhani, Alexis Moreno, Magda Teixeira Nunes, Lucia Gonzalez-Lobato, et al.. Uncompetitive nanomolar dimeric indenoindole inhibitors of the human breast cancer resistance pump ABCG2. European Journal of Medicinal Chemistry, Elsevier, 2020, pp.113017. ⟨10.1016/j.ejmech.2020.113017⟩. ⟨hal-03032952⟩
  • Saddam Charaabi, Rafik Absi, Anne-Marie Pensé-Lhéritier, Marc Le Borgne, Samar Issa. Adsorption studies of benzophenone-3 onto clay minerals and organosilicates: Kinetics and modelling. Applied Clay Science, Elsevier, 2020, pp.105937. ⟨10.1016/j.clay.2020.105937⟩. ⟨hal-03088439⟩
  • Isabelle Lengers, Fabian Herrmann, Marc Le Borgne, Joachim Jose. Improved Surface Display of Human Hyal1 and Identification of Testosterone Propionate and Chicoric Acid as New Inhibitors. Pharmaceuticals, MDPI, 2020, 13 (4), pp.54. ⟨10.3390/ph13040054⟩. ⟨hal-02539544⟩
  • Laurent Ettouati, Zoé Senta-Loys, Sandrine Bourgeois, Bernard Fenet, Marc Le Borgne, et al.. Behaviour of Tetrabenazine in Acid Medium: Reassessment and Impact on Formulation. Pharmaceutics, MDPI, 2019, 11 (1), pp.44. ⟨10.3390/pharmaceutics11010044⟩. ⟨hal-01987081⟩
  • Benoît Bestgen, Irina Kufareva, Weiguang Seetoh, Chris Abell, Rolf Hartmann, et al.. 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. Journal of Medicinal Chemistry, American Chemical Society, 2019, 62 (4), pp.1817-1836. ⟨10.1021/acs.jmedchem.8b01765⟩. ⟨hal-02465880⟩
  • Geir Kildahl-Andersen, Christian Schnaars, Anthony Prandina, Sylvie Radix, Marc Le Borgne, et al.. Synthesis and biological evaluation of zinc chelating compounds as metallo-β-lactamase inhibitors. MedChemComm, Royal Society of Chemistry, In press, 10 (4), pp.528-537. ⟨10.1039/C8MD00578H⟩. ⟨hal-02077900⟩
  • Saddam Charaabi, Lucien Tchara, Christelle Marminon, Zouhair Bouaziz, Gérard Holtzinger, et al.. A comparative adsorption study of benzophenone-3 onto synthesized lipophilic organosilicate, Laponite and montmorillonite. Applied Clay Science, Elsevier, 2019, 170, pp.114-124. ⟨10.1016/j.clay.2019.01.005⟩. ⟨hal-02004994⟩
  • Ghina Alameh, Agnès Emptoz-Bonneton, Marc Rolland de Ravel, Eva Matera, Elisabeth Mappus, et al.. 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. Journal of Enzyme Inhibition and Medicinal Chemistry, Informa Healthcare, 2019, 34 (1), pp.684-691. ⟨10.1080/14756366.2019.1575825⟩. ⟨hal-02077612⟩
  • Benoît Bestgen, Irina Kufareva, Weiguang Seetoh, Chris Abell, Rolf Hartmann, et al.. 2-Aminothiazole derivatives as selective allosteric modulators of the protein kinase CK2. Part 2: Structure–based optimization and investigation of effects specific to the allosteric mode of action. Journal of Medicinal Chemistry, American Chemical Society, 2019, 62 (4), pp.1817-1836. ⟨10.1021/acs.jmedchem.8b01765⟩. ⟨hal-02004987⟩
  • Dirk Lindenblatt, Anna Nickelsen, Violetta Applegate, Jennifer Hochscherf, Benedict Witulski, et al.. Diacritic Binding of an Indenoindole Inhibitor by CK2α Paralogs Explored by a Reliable Path to Atomic Resolution CK2α′ Structures. ACS Omega, ACS Publications, 2019, 4 (3), pp.5471-5478. ⟨10.1021/acsomega.8b03415⟩. ⟨hal-02077897⟩
  • Irina Kufareva, Benoît Bestgen, Paul Brear, Renaud Prudent, Béatrice Laudet, et al.. Discovery of holoenzyme-disrupting chemicals as substrate-selective CK2 inhibitors. Scientific Reports, Nature Publishing Group, 2019, 9 (1), pp.15893. ⟨10.1038/s41598-019-52141-5⟩. ⟨hal-02348673⟩
  • Caroline Bayart, Elisa Jean, Marie Paillagot, Alexia Renoud, Alice Raillard, et al.. Comparison of SEC and AF4 analytical tools for size estimation of typhoid Vi polysaccharides. Analytical Methods, Royal Society of Chemistry, 2019, ⟨10.1039/C9AY00145J⟩. ⟨hal-02288665⟩
  • Benoît Bestgen, Isabelle Krimm, Irina Kufareva, Ahmed Kamal, Wei Guang Seetoh, et al.. 2-Aminothiazole derivatives as selective allosteric modulators of the protein kinase CK2. Part 1: Identification of an allosteric binding site. Journal of Medicinal Chemistry, American Chemical Society, 2019, 62 (4), pp.1803-1816. ⟨10.1021/acs.jmedchem.8b01766⟩. ⟨hal-02004986⟩
  • Samar Issa, Anthony Prandina, Nicolas Bedel, Pal Rongved, Saïd Yous, et al.. Carbazole scaffolds in cancer therapy: a review from 2012 to 2018. Journal of Enzyme Inhibition and Medicinal Chemistry, Informa Healthcare, 2019, 34 (1), pp.1321-1346. ⟨10.1080/14756366.2019.1640692⟩. ⟨hal-02190476⟩
  • Claire Raingeval, Olivier Cala, Béatrice Brion, Marc Le Borgne, Roderick Eliot Hubbard, et al.. 1D NMR WaterLOGSY as an efficient method for fragment-based lead discovery. Journal of Enzyme Inhibition and Medicinal Chemistry, Informa Healthcare, 2019, 34 (1), pp.1218-1225. ⟨10.1080/14756366.2019.1636235⟩. ⟨hal-02188259⟩
  • Irina Kufareva, Benoît Bestgen, Paul Brear, Renaud Prudent, Béatrice Laudet, et al.. Discovery of holoenzyme-disrupting chemicals as substrate-selective CK2 inhibitors. Scientific Reports, Nature Publishing Group, 2019, 9 (1), ⟨10.1038/s41598-019-52141-5⟩. ⟨hal-02466039⟩
  • Anthony Prandina, Sylvie Radix, Marc Le Borgne, Lars Petter Jordheim, Zineb Bousfiha, et al.. Synthesis and biological evaluation of new dipicolylamine zinc chelators as metallo-β-lactamase inhibitors. Tetrahedron, Elsevier, 2019, 75 (11), pp.1525-1540. ⟨hal-02054167⟩
  • Christian Schnaars, Geir Kildahl-Andersen, Anthony Prandina, Roya Popal, Sylvie Large Radix, et al.. Synthesis and preclinical evaluation of TPA-based zinc chelators as metallo-β-lactamase inhibitors. ACS Infectious Diseases, American Chemical Society, 2018, ⟨10.1021/acsinfecdis.8b00137⟩. ⟨hal-01844562⟩
  • Mehdi Bouchouit, Sofiane Bouacida, Bachir Zouchoune, Hocine Merazig, Silvia Bua, et al.. Synthesis, X-ray structure, in silico calculation, and carbonic anhydrase inhibitory properties of benzylimidazole metal complexes. Journal of Enzyme Inhibition and Medicinal Chemistry, Informa Healthcare, 2018, 33 (1), pp.1150 - 1159. ⟨10.1080/14756366.2018.1481404⟩. ⟨hal-01839213⟩
  • Abdelhamid Nacereddine, Andre Bollacke, Eszter Roka, Christelle Marminon, Zouhair Bouaziz, et al.. Self-Assembled Supramolecular Nanoparticles Improve the Cytotoxic Efficacy of CK2 Inhibitor THN7. Pharmaceuticals, MDPI, 2018, 11 ((1)10), ⟨10.3390/ph11010010⟩. ⟨hal-01694352⟩
  • Abdeslem Bouzina, Khaoula Bechlem, Hajira Berredjem, Billel Belhani, Imène Becheker, et al.. Synthesis, Spectroscopic Characterization, and In Vitro Antibacterial Evaluation of Novel Functionalized Sulfamidocarbonyloxyphosphonates. Molecules, MDPI, 2018, 23 (7), ⟨10.3390/molecules23071682⟩. ⟨hal-01839215⟩
  • Sylwia Bloch, Bożena Nejman-Faleńczyk, Karolina Pierzynowska, Ewa Piotrowska, Alicja Węgrzyn, et al.. Inhibition of Shiga toxin-converting bacteriophage development by novel antioxidant compounds. Journal of Enzyme Inhibition and Medicinal Chemistry, Informa Healthcare, 2018, 33 (1), pp.639 - 650. ⟨10.1080/14756366.2018.1444610⟩. ⟨hal-01736468⟩
  • Anthony Prandina, Lars Herfindal, Sylvie Radix, Pal Rongved, Stein Døskeland, et al.. Enhancement of iodinin solubility by encapsulation into cyclodextrin nanoparticles. Journal of Enzyme Inhibition and Medicinal Chemistry, Informa Healthcare, 2018, 33 (1), pp.370 - 375. ⟨10.1080/14756366.2017.1421638⟩. ⟨hal-01688994⟩
  • Florian Braun, Nicole Bertoletti, Gabriele Möller, Jerzy Adamski, Martin Frotscher, et al.. Structure-based design and profiling of novel 17β-HSD14 inhibitors. European Journal of Medicinal Chemistry, Elsevier, 2018, 155, pp.61-76. ⟨10.1016/j.ejmech.2018.05.029⟩. ⟨hal-01801297⟩
  • Caroline Bayart, Sébastien Peronin, Elisa Jean, Joseph Paladino, Philippe Talaga, et al.. The combined use of analytical tools for exploring tetanus toxin and tetanus toxoid structures. Journal of Chromatography B - Analytical Technologies in the Biomedical and Life Sciences, Elsevier, 2017, 1054, pp.80 - 92. ⟨10.1016/j.jchromb.2017.04.009⟩. ⟨hal-01683240⟩
  • Saddam Charaabi, Pata-Eting Tchara, Zouhair Bouaziz, Christelle Marminon, Gérard Holtzinger, et al.. Ebisilc® Organosilicate Particles for Innovative Galenic Formulation. Annals of Pharmacology and Pharmaceutics, Remedy Publications LLC, 2017, 2(20), pp.1103. ⟨hal-01806454⟩
  • Samer Haidar, Zouhair Bouaziz, Christelle Marminon, Tuomo Laitinen, Antti Poso, et al.. Development of Pharmacophore Model for Indeno[1,2-b]indoles as Human Protein Kinase CK2 Inhibitors and Database Mining. Pharmaceuticals, MDPI, 2017, An Updated View on an Emerging Target: Selected Papers from the 8th International Conference on Protein Kinase CK2, 10 ((1)8), ⟨10.3390/ph10010008⟩. ⟨hal-01683291⟩
  • Esma Lamera, Sofiane Bouacida, Marc Le Borgne, Zouhair Bouaziz, Abdelmalek Bouraiou. Sequential MCR/Fisher indolization strategy for the construction of polycyclic carbazole derivatives. Tetrahedron Letters, Elsevier, 2017, 58 (13), pp.1305 - 1307. ⟨10.1016/j.tetlet.2017.02.047⟩. ⟨hal-01683348⟩
  • Esma Lamera, Sofiane Bouacida, Hocine Merazig, Aïssa Chibani, Marc Le Borgne, et al.. DMAP as a new efficient catalyst for the one-pot synthesis of condensed phthalazines. Zeitschrift fur Naturforschung B, Verlag der Zeitschrift Fuer Naturforschung, 2017, 72 ((5)b), pp.361-368. ⟨10.1515/znb-2016-0262⟩. ⟨hal-01683401⟩
  • Benoît Bestgen, Zakia Belaid-Choucair, Thierry Lomberget, Marc Le Borgne, Odile Filhol, et al.. In Search of Small Molecule Inhibitors Targeting the Flexible CK2 Subunit Interface. Pharmaceuticals, MDPI, 2017, An Updated View on an Emerging Target: Selected Papers from the 8th International Conference on Protein Kinase CK2, 10 ((1)16), ⟨10.3390/ph10010016⟩. ⟨hal-01683243⟩
  • Joachim Jose, Marc Le-Borgne, Lorenzo Pinna, Mathias Montenarh. Editorial: An Updated View on an Emerging Target: Selected Papers from the 8th International Conference on Protein Kinase CK2. Pharmaceuticals, MDPI, 2017, Pharmaceuticals, 10 ((2)33), pp.33 - 33. ⟨10.3390/ph10020033⟩. ⟨hal-01683242⟩
  • Jennifer Hochscherf, Dirk Lindenblatt, Benedict Witulski, Robin Birus, Dagmar Aichele, et al.. 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′. Pharmaceuticals, MDPI, 2017, 10 ((4)98), ⟨10.3390/ph10040098⟩. ⟨hal-01683237⟩
  • Anaïs Goudard, Laure Lalande, Camille Bertin, Marie Sautereau, Marc Le Borgne, et al.. Sleep Disorders and Therapeutic Management: A Survey in a French Population of Prisoners. Journal of Correctional Health Care, SAGE Publications, 2017, 23 (2), pp.193 - 202. ⟨10.1177/1078345817700163⟩. ⟨hal-01683241⟩
  • Andre Bollacke, Christian Nienberg, Marc Le Borgne, Joachim Jose. Toward selective CK2alpha and CK2alpha’ inhibitors: Development of a novel whole-cell kinase assay by Autodisplay of catalytic CK2alpha’. Journal of Pharmaceutical and Biomedical Analysis, Elsevier, 2016, 121, pp.253 - 260. ⟨10.1016/j.jpba.2016.01.011⟩. ⟨hal-01683296⟩
  • Nathalie Guragossian, Gustavo Jabor Gozzi, Bruno Fouillet, Marie-Paule Gustin, Raphaël Terreux, et al.. Candidate Molecule Selection Based on In Silico Predicted ADMET Properties of 12 Indenoindole Derivatives. Chemical Informatics, iMedPub Journals, 2016, 2 ((2)6), ⟨10.21767/2470-6973.100020⟩. ⟨hal-01683399⟩
  • Elisabeta Baiceanu, Kim-Anh Nguyen, Lucia Gonzalez-Lobato, Rachad Nasr, Hélène Baubichon-Cortay, et al.. 2-Indolylmethylenebenzofuranones as first effective inhibitors of ABCC2. European Journal of Medicinal Chemistry, Elsevier, 2016, 122, pp.408 - 418. ⟨10.1016/j.ejmech.2016.06.039⟩. ⟨hal-01683292⟩
  • Faten Alchab, Estelle Sibille, Laurent Ettouati, Emilie Bana, Zouhair Bouaziz, et al.. Screening of indeno[1,2- b]indoloquinones by MALDI-MS: a new set of potential CDC25 phosphatase inhibitors brought to light. Journal of Enzyme Inhibition and Medicinal Chemistry, Informa Healthcare, 2016, 31 (sup3), pp.25 - 32. ⟨10.1080/14756366.2016.1201480⟩. ⟨hal-01655213⟩
  • Gustavo Jabor Gozzi, Zouhair Bouaziz, Evelyn Winter, Nathalia Daflon-Yunes, Mylène Honorat, et al.. Phenolic indeno[1,2-b]indoles as ABCG2-selective potent and non-toxic inhibitors stimulating basal ATPase activity.. Drug Design, Development and Therapy, Dove Medical Press, 2015, 9, pp.3481-3495. ⟨10.2147/DDDT.S84982⟩. ⟨hal-01179426⟩
  • Marc Rolland de Ravel, Ghina Alameh, Maxime Melikian, Zahia Mahiout, Agnès Emptoz-Bonneton, et al.. Synthesis of New Steroidal Inhibitors of P-Glycoprotein-Mediated Multidrug Resistance and Biological Evaluation on K562/R7 Erythroleukemia Cells. Journal of Medicinal Chemistry, American Chemical Society, 2015, 58 (4), pp.1832 - 1845. ⟨10.1021/jm501676v⟩. ⟨hal-01683301⟩
  • Gustavo Jabor Gozzi, Zouhair Bouaziz, Evelyn Winter, Nathalia Daflon-Yunes, Dagmar Aichele, et al.. Converting potent indeno[1,2-b]indole inhibitors of protein kinase CK2 into selective inhibitors of the breast cancer resistance protein ABCG2. Journal of Medicinal Chemistry, American Chemical Society, 2015, 58 (1), pp.265-77. ⟨10.1021/jm500943z⟩. ⟨hal-01174925⟩
  • Florine Lecerf-Schmidt, Romain Haudecoeur, Basile Peres, Marc Ferreira Queiroz, Marc Marcourt, et al.. Biomimetic synthesis of Tramadol. Chemical Communications, Royal Society of Chemistry, 2015, 51 (77), pp.14451 - 14453. ⟨10.1039/c5cc05948h⟩. ⟨hal-01683298⟩
  • Esma Lamera, Saida Benzerka, Abdelmalek Bouraiou, Sofiane Bouacida, Hocine Merazig, et al.. Crystal structure of 13-phenyl-2,3,4,13-tetrahydro-1 H -indazolo[1,2- b ]phthalazine-1,6,11-trione. Acta crystallographica. Section E, Crystallographic communications, International Union of Crystallography, 2015, 71 (12), pp.o1036 - o1037. ⟨10.1107/S2056989015023452⟩. ⟨hal-01683294⟩
  • Christelle Marminon, Abdelhamid Nacereddine, Zouhair Bouaziz, Pascal Nebois, Joachim Jose, et al.. Microwave-assisted oxidation of indan-1-ones into ninhydrins. Tetrahedron Letters, Elsevier, 2015, 56 (14), pp.1840 - 1842. ⟨10.1016/j.tetlet.2015.02.086⟩. ⟨hal-01683347⟩
  • Christophe Neyra, Joseph Paladino, Marc Le Borgne. Mechanisms of depolymerization and activation of a polysialic acid and its tetramer by hydrogen peroxide. Carbohydrate Polymers, Elsevier, 2015, 115, pp.494 - 501. ⟨10.1016/j.carbpol.2014.08.112⟩. ⟨hal-01683316⟩
  • Billel Belhani, Malika Berredjem, Marc Le Borgne, Zouhair Bouaziz, Jacques Lebreton, et al.. A one-pot three-component synthesis of novel α-sulfamidophosphonates under ultrasound irradiation and catalyst-free conditions. RSC Advances, Royal Society of Chemistry, 2015, 5 (49), pp.39324 - 39329. ⟨10.1039/C5RA03473F⟩. ⟨hal-01694993⟩
  • Andre Gratz, Andre Bollacke, Sara Stephan, Christian Nienberg, Marc Le Borgne, et al.. Functional display of heterotetrameric human protein kinase CK2 on Escherichia coli: a novel tool for drug discovery. Microbial Cell Factories, BioMed Central, 2015, 14 (74), ⟨10.1186/s12934-015-0263-z⟩. ⟨hal-01683300⟩
  • Zouhair Bouaziz, Samar Issa, Jacques Gentili, Andre Gratz, Andre Bollacke, et al.. Biologically active carbazole derivatives: focus on oxazinocarbazoles and related compounds. Journal of Enzyme Inhibition and Medicinal Chemistry, Informa Healthcare, 2015, 30 (2), pp.180 - 188. ⟨10.3109/14756366.2014.899594⟩. ⟨hal-01683306⟩
  • Faten Alchab, Laurent Ettouati, Zouhair Bouaziz, Andre Bollacke, Jean-Guy Delcros, et al.. Synthesis, Biological Evaluation and Molecular Modeling of Substituted Indeno[1,2-b]indoles as Inhibitors of Human Protein Kinase CK2.. Pharmaceuticals, MDPI, 2015, 8 (2), pp.279-302. ⟨10.3390/ph8020279⟩. ⟨hal-01164133⟩
  • Zouaoui Bourezg, Nathalie Cartiser, Laurent Ettouati, Jean Guillon, Aline Lacoudre, et al.. Structural elucidation of two photolytic degradation products of tetrabenazine. Journal of Pharmaceutical and Biomedical Analysis, Elsevier, 2014, 91, pp.138 - 143. ⟨10.1016/j.jpba.2013.12.032⟩. ⟨hal-01655151⟩
  • Julien Defaux, Maud Antoine, Cédric Logé, Marc Le Borgne, Tilmann Schuster, et al.. 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. Bioorganic and Medicinal Chemistry Letters, Elsevier, 2014, 24 (16), pp.3748 - 3752. ⟨10.1016/j.bmcl.2014.06.078⟩. ⟨hal-01683305⟩
  • Julien Defaux, Maud Antoine, Marc Le Borgne, Tilmann Schuster, Irene Seipelt, et al.. Discovery of 7-Aryl-Substituted (1,5-Naphthyridin-4-yl)ureas as Aurora Kinase Inhibitors. ChemMedChem, Wiley-VCH Verlag, 2014, 9 (1), pp.217 - 232. ⟨10.1002/cmdc.201300384⟩. ⟨hal-01683307⟩
  • Christophe Neyra, Joseph Paladino, Marc Le Borgne. Oxidation of sialic acid using hydrogen peroxide as a new method to tune the reducing activity. Carbohydrate Research, Elsevier, 2014, 386, pp.92 - 98. ⟨10.1016/j.carres.2014.01.007⟩. ⟨hal-01683314⟩
  • Géraldine Agusti, Sandrine Bourgeois, Nathalie Cartiser, Hatem Fessi, Marc Le Borgne, et al.. A safe and practical method for the preparation of 7α-thioether and thioester derivatives of spironolactone. Steroids, Elsevier, 2013, 78 (1), pp.102 - 107. ⟨10.1016/j.steroids.2012.09.005⟩. ⟨hal-01683309⟩
  • Ahcène Boumendjel, Germain Sotoing Taïwe, Elisabeth Ngo Gum, Tanguy Chabrol, Chantal Beney, et al.. African tree gets to the root of pain. Nature, Nature Publishing Group, 2013, 501 (7467), pp.285 - 285. ⟨10.1038/501285b⟩. ⟨hal-01683403⟩
  • Florent Perret, Christelle Marminon, Wael Zeinyeh, Pascal Nebois, Andre Bollacke, et al.. Preparation and characterization of CK2 inhibitor-loaded cyclodextrin nanoparticles for drug delivery. International Journal of Pharmaceutics, Elsevier, 2013, 441 (1-2), pp.491 - 498. ⟨10.1016/j.ijpharm.2012.11.004⟩. ⟨hal-01683336⟩
  • Jean Guillon, Marc Le Borgne, Charlotte Rimbault, Stéphane Moreau, Solène Savrimoutou, et al.. Synthesis and biological evaluation of novel substituted pyrrolo[1,2-a]quinoxaline derivatives as inhibitors of the human protein kinase CK2. European Journal of Medicinal Chemistry, Elsevier, 2013, 65, pp.205 - 222. ⟨10.1016/j.ejmech.2013.04.051⟩. ⟨hal-01683308⟩
  • Faten Al Chab, Bernard Fenet, Marc Le Borgne, Joachim Jose, Noël Pinaud, et al.. 1H and 13C NMR assignments of bioactive indeno[1,2-b]indole-10-one derivatives. Magnetic Resonance in Chemistry, Wiley, 2013, 51 (12), pp.837 - 841. ⟨10.1002/mrc.4016⟩. ⟨hal-01655126⟩
  • Pal Rongved, Gilbert Kirsch, Zouhair Bouaziz, Joachim Jose, Marc Le Borgne. Indenoindoles and cyclopentacarbazoles as bioactive compounds: Synthesis and biological applications. European Journal of Medicinal Chemistry, Elsevier, 2013, 69, pp.465 - 479. ⟨10.1016/j.ejmech.2013.08.049⟩. ⟨hal-01524692⟩
  • Ahcène Boumendjel, Germain Sotoing Taïwe, Elisabeth Ngo Bum, Tanguy Chabrol, Chantal Beney, et al.. Occurrence of the Synthetic Analgesic Tramadol in an African Medicinal Plant.. Angewandte Chemie International Edition, Wiley-VCH Verlag, 2013, 52 (45), pp.11780-4. ⟨10.1002/anie.201305697⟩. ⟨inserm-00874145⟩
  • Claas Hundsdörfer, Hans-Jörg Hemmerling, Janina Hamberger, Marc Le Borgne, Patrick Bednarski, et al.. Novel indeno[1,2-b]indoloquinones as inhibitors of the human protein kinase CK2 with antiproliferative activity towards a broad panel of cancer cell lines. Biochemical and Biophysical Research Communications, Elsevier, 2012, 424 (1), pp.71 - 75. ⟨10.1016/j.bbrc.2012.06.068⟩. ⟨hal-01683311⟩
  • Claas Hundsdörfer, Hans-Jörg Hemmerling, Claudia Götz, Frank Totzke, Patrick Bednarski, et al.. Indeno[1,2-b]indole derivatives as a novel class of potent human protein kinase CK2 inhibitors. Bioorganic and Medicinal Chemistry, Elsevier, 2012, 20 (7), pp.2282 - 2289. ⟨10.1016/j.bmc.2012.02.017⟩. ⟨hal-01683312⟩
  • Rémi Guillon, Fabrice Pagniez, Francis Giraud, Damien Crépin, Carine Picot, et al.. 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. ChemMedChem, Wiley-VCH Verlag, 2011, 6 (5), pp.816 - 825. ⟨10.1002/cmdc.201000530⟩. ⟨hal-01689176⟩
  • Francis Giraud, Cédric Logé, Fabrice Pagniez, Damien Crepin, Sophie Barres, et al.. Design, synthesis and evaluation of 3-(imidazol- 1-ylmethyl)indoles as antileishmanial agents. Part II. Journal of Enzyme Inhibition and Medicinal Chemistry, Informa Healthcare, 2009, 24 (5), pp.1067 - 1075. ⟨10.1080/14756360802610795⟩. ⟨hal-01689191⟩
  • Rémi Guillon, Francis Giraud, Cédric Logé, Marc Le Borgne, Carine Picot, et al.. 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. Bioorganic and Medicinal Chemistry Letters, Elsevier, 2009, 19 (20), pp.5833 - 5836. ⟨10.1016/j.bmcl.2009.08.089⟩. ⟨hal-01689189⟩
  • Francis Giraud, Rémi Guillon, Cédric Logé, Fabrice Pagniez, Carine Picot, et al.. 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. Bioorganic and Medicinal Chemistry Letters, Elsevier, 2009, 19 (2), pp.301 - 304. ⟨10.1016/j.bmcl.2008.11.101⟩. ⟨hal-01689192⟩
  • Marie-Pierre Lézé, Anja Palusczak, Rolf W Hartmann, Marc Le Borgne. Synthesis of 6- or 4-functionalized indoles via a reductive cyclization approach and evaluation as aromatase inhibitors. Bioorganic and Medicinal Chemistry Letters, Elsevier, 2008, 18 (16), pp.4713 - 4715. ⟨10.1016/j.bmcl.2008.06.094⟩. ⟨hal-01689195⟩
  • Francis Giraud, Cédric Logé, Fabrice Pagniez, Damien Crepin, Patrice Le Pape, et al.. Design, synthesis, and evaluation of 1-(N-benzylamino)-2-phenyl-3-(1H-1,2,4-triazol-1-yl)propan-2-ols as antifungal agents. Bioorganic and Medicinal Chemistry Letters, Elsevier, 2008, 18 (6), pp.1820 - 1824. ⟨10.1016/j.bmcl.2008.02.027⟩. ⟨hal-01689196⟩
  • Marc Le Borgne, Pascal Marchand, Marie-Renée Nourrisson, Denis Loquet, Martina Palzer, et al.. Synthesis and biological evaluation of 3-(azolylmethyl)-1 H -indoles and 3-(α-azolylbenzyl)-1 H -indoles as selective aromatase inhibitors. Journal of Enzyme Inhibition and Medicinal Chemistry, Informa Healthcare, 2007, 22 (5), pp.667 - 676. ⟨10.1080/14756360701652658⟩. ⟨hal-01689199⟩
  • Nicolas Lebouvier, Fabrice Pagniez, Muriel Duflos, Patrice Le Pape, Young Min Na, et al.. Synthesis and antifungal activities of new fluconazole analogues with azaheterocycle moiety. Bioorganic and Medicinal Chemistry Letters, Elsevier, 2007, 17 (13), pp.3686 - 3689. ⟨10.1016/j.bmcl.2007.04.038⟩. ⟨hal-01689197⟩
  • Nicolas Lebouvier, Francis Giraud, Typhanie Corbin, Young Min Na, Guillaume Le Baut, et al.. Efficient microwave-assisted synthesis of 1-(1H-indol-1-yl)-2-phenyl-3-(1H-1,2,4-triazol-1-yl)propan-2-ols as antifungal agents. Tetrahedron Letters, Elsevier, 2006, 47 (36), pp.6479 - 6483. ⟨10.1016/j.tetlet.2006.03.199⟩. ⟨hal-01689208⟩
  • Marie-Pierre Lézé, Marc Le Borgne, Patricia Pinson, Anja Palusczak, Muriel Duflos, et al.. Synthesis and biological evaluation of 5-[(aryl)(1H-imidazol-1-yl)methyl]-1H-indoles: Potent and selective aromatase inhibitors. Bioorganic and Medicinal Chemistry Letters, Elsevier, 2006, 16 (5), pp.1134 - 1137. ⟨10.1016/j.bmcl.2005.11.099⟩. ⟨hal-01689230⟩
  • Francis Giraud, Cédric Loge, Marc Le Borgne, Francis Pagniez, Young Min Na, et al.. A 3D-QSAR CoMSIA study on 3-azolylmethylindoles as anti-leishmanial agents. SAR and QSAR in Environmental Research, Taylor & Francis, 2006, 17 (3), pp.299 - 309. ⟨10.1080/10659360600787494⟩. ⟨hal-01689291⟩
  • Fabrice Pagniez, Hiam Abdala-Valencia, Pascal Marchand, Marc Le Borgne, Guillaume Le Baut, et al.. Antileishmanial activities and mechanisms of action of indole-based azoles. Journal of Enzyme Inhibition and Medicinal Chemistry, Informa Healthcare, 2006, 21 (3), pp.277 - 283. ⟨10.1080/14756360600700517⟩. ⟨hal-01689215⟩
  • Cédric Logé, Marc Le Borgne, Pascal Marchand, Jean-Michel Robert, Guillaume Le Baut, et al.. Three-dimensional model of cytochrome P450 human aromatase. Journal of Enzyme Inhibition and Medicinal Chemistry, Informa Healthcare, 2005, 20 (6), pp.581 - 585. ⟨10.1080/14756360500220574⟩. ⟨hal-01689233⟩
  • Marie-Pierre Lézé, Marc Le Borgne, Pascal Marchand, Denis Loquet, Manuela Kogler, et al.. 2- and 3-[(Aryl)(azolyl)methyl]indoles as Potential Non-steroidal Aromatase Inhibitors. Journal of Enzyme Inhibition and Medicinal Chemistry, Informa Healthcare, 2004, 19 (6), pp.549 - 557. ⟨10.1080/14756360400004631⟩. ⟨hal-01689238⟩
  • Young Min Na, Nicolas Lebouvier, Marc Le Borgne, Fabrice Pagniez, Nidia Alvarez, et al.. Synthesis and Antileishmanial Activity of 3-Imidazolylalkylindoles. Part I. Journal of Enzyme Inhibition and Medicinal Chemistry, Informa Healthcare, 2004, 19 (6), pp.451 - 457. ⟨10.1080/14756360412331280509⟩. ⟨hal-01689240⟩
  • Young Na, Marc Le Borgne, Fabrice Pagniez, Guillaume Le Baut, Patrice Le Pape. Synthesis and antifungal activity of new 1-halogenobenzyl-3-imidazolylmethylindole derivatives. European Journal of Medicinal Chemistry, Elsevier, 2003, 38 (1), pp.75 - 87. ⟨10.1016/S0223-5234(02)00005-3⟩. ⟨hal-01689264⟩
  • Pascal Marchand, Marc Le Borgne, Martina Palzer, Guillaume Le Baut, Rolf Hartmann. Preparation and pharmacological profile of 7-(α-Azolylbenzyl)-1H-indoles and indolines as new aromatase inhibitors. Bioorganic and Medicinal Chemistry Letters, Elsevier, 2003, 13 (9), pp.1553 - 1555. ⟨10.1016/S0960-894X(03)00182-3⟩. ⟨hal-01689266⟩
  • Marc Le Borgne, Pascal Marchand, Guillaume Le Baut, Masoud Ahmadi, H. John Smith, et al.. Retinoic Acid Metabolism Inhibition by 3-Azolylmethyl-1 H -indoles and 2, 3 or 5-(α-Azolylbenzyl)-1 H -indoles. Journal of Enzyme Inhibition and Medicinal Chemistry, Informa Healthcare, 2003, 18 (2), pp.155 - 158. ⟨10.1080/1475636032000069819⟩. ⟨hal-01689267⟩
  • Fabrice Pagniez, Marc Le Borgne, Pascal Marchand, Young Min Na, Guillaume Le Baut, et al.. In Vitro Activity of a New Antifungal Azolyl-substituted Indole Against Aspergillus fumigatus. Journal of Enzyme Inhibition and Medicinal Chemistry, Informa Healthcare, 2002, 17 (6), pp.425 - 429. ⟨10.1080/1475636021000005686⟩. ⟨hal-01689259⟩
  • Pascal Marchand, Marc Le Borgne, Young Min Na, Fabrice Pagniez, Hiam Abdala, et al.. Synthesis and Antileishmanial Activity of 3-(α-Azolylbenzyl)indoles. Journal of Enzyme Inhibition and Medicinal Chemistry, Informa Healthcare, 2002, 17 (6), pp.353 - 358. ⟨10.1080/1475636021000005613⟩. ⟨hal-01689261⟩
  • Christine Pato, Marc Le Borgne, Guillaume Le Baut, Patrice Le Pape, Didier Marion, et al.. Potential application of plant lipid transfer proteins for drug delivery. Biochemical Pharmacology, Elsevier, 2001, 62 (5), pp.555 - 560. ⟨10.1016/S0006-2952(01)00708-0⟩. ⟨hal-01689248⟩
  • Marc Le Borgne, Muriel Duflos, Guillaume Le Baut, Paul Nicholls. Dérivés indoliques à activités anti-inflammatoire ou antitumorale. Annales Pharmaceutiques Françaises, Elsevier Masson, 2000, 58 (5), pp.316 - 320. ⟨hal-01689246⟩
  • Marc Le Borgne, Pascal Marchand, Bénédicte Delevoye-Seiller, Jean-Michel Robert, Guillaume Le Baut, et al.. New selective nonsteroidal aromatase inhibitors: Synthesis and inhibitory activity of 2,3 or 5-(α-azolylbenzyl)-1H-indoles. Bioorganic and Medicinal Chemistry Letters, Elsevier, 1999, 9 (3), pp.333 - 336. ⟨10.1016/S0960-894X(98)00737-9⟩. ⟨hal-01689251⟩
  • Pascal Marchand, Marc Le Borgne, Muriel Duflos, Sylvie Piessard-Robert, Guillaume Le Baut, et al.. 3-(Azolylmethyl)-1H-indoles as Selective P450 Aromatase Inhibitors. Pharmacy and Pharmacology Communications, Royal Pharmaceutical Society of Great Britain, 1998, 4 (4), pp.211 - 218. ⟨10.1111/j.2042-7158.1998.tb00337.x⟩. ⟨hal-01689256⟩
  • Marc Le Borgne, Pascal Marchand, Muriel Duflos, Bénédicte Delevoye-Seiller, Sylvie Piessard-Robert, et al.. Synthesis andIn Vitro Evaluation of 3-(1-Azolylmethyl)-1H-indoles and 3-(1-Azolyl-1-phenylmethyl)-1H-indoles as Inhibitors of P450 arom. Archiv der Pharmazie / Chemistry in Life Sciences, Wiley-VCH Verlag, 1997, 330 (5), pp.141 - 145. ⟨10.1002/ardp.19973300506⟩. ⟨hal-01689244⟩
  • Marc Le Borgne, Pascal Marchand, Muriel Duflos, Sylvie Piessard-Robert, Guillaume Le Baut, et al.. Comparison of the In-vitro Aromatase Inhibitory Activity of 3-(Azolylmethyl)-1H-indoles. Pharmacy and Pharmacology Communications, Royal Pharmaceutical Society of Great Britain, 1997, 3 (5-6), pp.279 - 281. ⟨10.1111/j.2042-7158.1997.tb00264.x⟩. ⟨hal-01689254⟩

Conference papers6 documents

  • Robin Birus, Marc Le Borgne, Joachim Jose. Investigation of pharmacokinetic properties of CK2 Inhibitors with an Indeno[1,2-b]indole scaffold. 5th International Electronic Conference on Medicinal Chemistry, Nov 2019, Basel, Switzerland. ⟨hal-02480385⟩
  • Isadora da Silva Zanzarini, Esma Lamera, Sofiane Bouacida, Ingrid Zattoni, Diogo Henrique Kita, et al.. Design, Synthesis, X-ray Structure and Evaluation of Functionalized Hexacyclic Carbazoles as New Inhibitors of ABCG2 Transporter. 5th International Electronic Conference on Medicinal Chemistry, Nov 2019, Basel, Switzerland. ⟨hal-02480387⟩
  • Joachim Jose, Marc Le Borgne, Karsten Niefind. 25th Conference of GP2A: From Selective, Bivalent Inhibitors to Multi-Target Drugs by the Example of Human Protein Kinase CK2, an Emerging Cancer Target. 25th Conference of GP2A, Aug 2017, Liverpool, United Kingdom. pp.9-10/2.12, ⟨10.3390/ph10040097⟩. ⟨hal-01683410⟩
  • Samer Haidar, Zouhair Bouaziz, Christelle Marminon, Tiomo Laitinen, Anti Poso, et al.. Development of Pharmacophore Model for Indeno[1,2-b]indoles as Human Protein Kinase CK2 Inhibitors and Database Mining. 3rd International Electronic Conference on Medicinal Chemistry, Nov 2017, Basel, Switzerland. ⟨hal-02480388⟩
  • Dagmar Aichele, Marc Le Borgne, Joachim Jose. Indeno[1,2-b]indole Inhibitors of Human Protein Kinase CK2 and Their Impact on Different Tumor Cell Lines (A021). Second International Electronic Conference on Medicinal Chemistry (ECMC-2), Nov 2016, Bâle, Switzerland. pp.15/A021, ⟨10.3390/ph10010020⟩. ⟨hal-01683452⟩
  • Laurent Ettouati, Marie-Emmanuelle Million, Ophélie Arnaud, Géraldine Agusti, Waël Zeinyeh, et al.. Advances in peptidomimetics as inhibitors of ABC transporters. 1st International Electronic Conference on Medicinal Chemistry, Nov 2015, sciforum.net, France. ⟨10.3390/ecmc-1-A043⟩. ⟨hal-01710182⟩

Books1 document

  • Joachim Jose, Marc Le Borgne, Lorenzo Pinna, Mathias Montenarh. An Updated View on an Emerging Target: Selected Papers from the 8 th International Conference on Protein Kinase CK2. MDPI AG, 2017, 978-3-03842-413-0. ⟨hal-01700408⟩

Directions of work or proceedings3 documents

  • Marc Le Borgne, Samer Haidar, Olivier Duval, Bernhard Wünsch, Joachim Jose. 1st Joint European Conference on Therapeutic Targets and Medicinal Chemistry (TTMC 2015). Aug 2015, Muenster, France. Pharmaceuticals, 9 ((1)1), 2015, Pharmaceuticals, ⟨10.3390/ph9010001⟩. ⟨hal-01683297⟩
  • Zouhair Bouaziz, Samar Issa, Marc Le Borgne, Joachim Jose, Andreas Gratz, et al.. 81: Targeting casein kinase 2 in drug discovery: identification of new chemical entities. Bulletin du Cancer, 97 (1(Supplement)), pp.S68-S69, 2010, Échappement Tumoral, ⟨10.1684/bdc.2010.1058⟩. ⟨hal-01691315⟩
  • Jean Guillon, Guillaume Le Baut, Marc Le Borgne. Proceedings of the 16th annual conference of the Groupement des Pharmacochimistes de l'Arc Atlantique (GP2A). 16th GP2A, Sep 2007, Bordeaux, France. Journal of Enzyme Inhibition and Medicinal Chemistry, 23 (5), pp.587 - 587, 2008, 16th GP2A, ⟨10.1080/14756360802204656⟩. ⟨hal-01689205⟩