Cedric Loge

Summary

Country: France

Publications

  1. ncbi request reprint Three-dimensional model of cytochrome P450 human aromatase
    Cedric Loge
    Department de Pharmacochimie, Biomolécules et Cibles Thérapeutiques, UPRES EA1155, UFR Sciences Pharmaceutiques, 1 rue Gaston Veil, F 44035 Nantes Cedex 1, France
    J Enzyme Inhib Med Chem 20:581-5. 2005
  2. ncbi request reprint Novel 9-oxo-thiazolo[5,4-f]quinazoline-2-carbonitrile derivatives as dual cyclin-dependent kinase 1 (CDK1)/glycogen synthase kinase-3 (GSK-3) inhibitors: synthesis, biological evaluation and molecular modeling studies
    Cedric Loge
    Universite de Nantes, Nantes Atlantique Universites, Biomolécules et Cibles Thérapeutiques, Departement de Pharmacochimie, BioCiT, UPRES EA 1155, UFR Sciences Pharmaceutiques, Nantes Cedex 1, France
    Eur J Med Chem 43:1469-77. 2008
  3. doi request reprint 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
    Rémi Guillon
    Universite de Nantes, Nantes Atlantique Universites, Departement de Pharmacochimie, Cibles et Médicaments des Infections, de l Immunité et du Cancer, IICIMED EA 1155, UFR Sciences Pharmaceutiques, Nantes, France
    ChemMedChem 6:816-25. 2011
  4. doi request reprint Design, synthesis, and biological evaluation of 1-[(biarylmethyl)methylamino]-2-(2,4-difluorophenyl)-3-(1H-1,2,4-triazol-1-yl)propan-2-ols as potent antifungal agents: new insights into structure-activity relationships
    Rémi Guillon
    Universite de Nantes, Nantes Atlantique Universites, Departement de Pharmacochimie, Cibles et Médicaments des Infections de l Immunité et du Cancer, IICIMED EA 1155, UFR Sciences Pharmaceutiques, 1 rue Gaston Veil, Nantes 44035 Cedex 1, France
    ChemMedChem 6:1806-15. 2011
  5. doi request reprint 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
    Rémi Guillon
    Universite de Nantes, Nantes Atlantique Universites, Departement de Pharmacochimie, Cibles et Médicaments des Infections, de l Immunité et du Cancer, IICIMED EA 1155, UFR Sciences Pharmaceutiques, 1 rue Gaston Veil, Nantes F 44035 Cedex 1, France
    Bioorg Med Chem Lett 19:5833-6. 2009
  6. doi request reprint Synthesis and in vitro antifungal evaluation of 2-(2,4-difluorophenyl)-1-[(1H-indol-3-ylmethyl)methylamino]-3-(1H-1,2,4-triazol-1-yl)propan-2-ols
    Rémi Guillon
    Universite de Nantes, Nantes Atlantique Universites, Departement de Pharmacochimie, Cibles et Médicaments des Infections, de l Immunité et du Cancer, IICIMED EA 1155, UFR Sciences Pharmaceutiques, Nantes, France
    J Enzyme Inhib Med Chem 26:261-9. 2011
  7. doi request reprint 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
    Francis Giraud
    Universite de Nantes, Nantes Atlantique Universites, Departement de Pharmacochimie, Cibles et Médicaments des Infections, de l Immunité et du Cancer, IICIMED EA 1155, UFR de Sciences Pharmaceutiques, 1 rue Gaston Veil, Nantes F 44035 Cedex 1, France
    Bioorg Med Chem Lett 19:301-4. 2009
  8. doi request reprint Design, synthesis and evaluation of 3-(imidazol- 1-ylmethyl)indoles as antileishmanial agents. Part II
    Francis Giraud
    Departement de Pharmacochimie, Cibles et Médicaments des Infections, de l Immunité et du Cancer, IICIMED EA 1155, UFR de Sciences Pharmaceutiques, Universite de Nantes, Nantes F 44000, France
    J Enzyme Inhib Med Chem 24:1067-75. 2009
  9. doi request reprint Synthesis of new pyridazino[4,5-b]indol-4-ones and pyridazin-3(2H)-one analogs as DYRK1A inhibitors
    Amélie Bruel
    Universite de Nantes, Nantes Atlantique Universites, Laboratoire de Chimie Therapeutique, Cibles et Médicaments des Infections et du Cancer, IICIMED EA 1155, UFR Sciences Pharmaceutiques, 1 rue Gaston Veil, Nantes F 44035 Cedex 1, France
    Bioorg Med Chem Lett 24:5037-40. 2014
  10. doi request reprint Synthesis and biological evaluation of new 5-benzylated 4-oxo-3,4-dihydro-5H-pyridazino[4,5-b]indoles as PI3Kα inhibitors
    Amélie Bruel
    Universite de Nantes, Nantes Atlantique Universites, Laboratoire de Chimie Therapeutique, Cibles et Médicaments des Infections et du Cancer, IICIMED EA 1155, UFR Sciences Pharmaceutiques, 1 rue Gaston Veil, Nantes F 44035 Cedex 1, France
    Eur J Med Chem 57:225-33. 2012

Collaborators

  • Patrice Le Pape
  • Marc Le Borgne
  • Francis Giraud
  • Florent Morio
  • Julien Farard
  • Rolf W Hartmann
  • L Meijer
  • Rémi Guillon
  • Amélie Bruel
  • Fabrice Pagniez
  • Carine Picot
  • Muriel Duflos
  • Julien Defaux
  • Myriam Ravache
  • Hélène Bénédetti
  • Remy Le Guevel
  • Jean Michel Robert
  • Olivier Lozach
  • Maud Antoine
  • Babette Aicher
  • Eckhard Gunther
  • Romain Bénéteau
  • Tilmann Schuster
  • Michael Teifel
  • Pascal Marchand
  • Irene Seipelt
  • Mylène Chabanne
  • Matthias Gerlach
  • Christiane Guillouzo
  • Jana Sopkova de Oliveira Santos
  • Marie Ludivine de Tauzia
  • Sandrine Ruchaud
  • Jean François Lohier
  • Charlotte Rambaud
  • Damien Crepin
  • Veronique Ferchaud-Roucher

Detail Information

Publications14

  1. ncbi request reprint Three-dimensional model of cytochrome P450 human aromatase
    Cedric Loge
    Department de Pharmacochimie, Biomolécules et Cibles Thérapeutiques, UPRES EA1155, UFR Sciences Pharmaceutiques, 1 rue Gaston Veil, F 44035 Nantes Cedex 1, France
    J Enzyme Inhib Med Chem 20:581-5. 2005
    ..In addition, this model is consistent with the recent combined mutagenesis/modeling studies already published concerning the roles ofAsp309 and His480 in the aromatization of the steroid A ring...
  2. ncbi request reprint Novel 9-oxo-thiazolo[5,4-f]quinazoline-2-carbonitrile derivatives as dual cyclin-dependent kinase 1 (CDK1)/glycogen synthase kinase-3 (GSK-3) inhibitors: synthesis, biological evaluation and molecular modeling studies
    Cedric Loge
    Universite de Nantes, Nantes Atlantique Universites, Biomolécules et Cibles Thérapeutiques, Departement de Pharmacochimie, BioCiT, UPRES EA 1155, UFR Sciences Pharmaceutiques, Nantes Cedex 1, France
    Eur J Med Chem 43:1469-77. 2008
    ..Combination of lead optimization and molecular modeling studies allowed identification of a dual CDK1/GSK-3 inhibitor (compound 13d) with submicromolar values...
  3. doi request reprint 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
    Rémi Guillon
    Universite de Nantes, Nantes Atlantique Universites, Departement de Pharmacochimie, Cibles et Médicaments des Infections, de l Immunité et du Cancer, IICIMED EA 1155, UFR Sciences Pharmaceutiques, Nantes, France
    ChemMedChem 6:816-25. 2011
    ..albicans isolates. Synthesis, investigation of the mechanism of action by sterol analysis in a C. albicans strain, and structure-activity relationships (SARs) are reported...
  4. doi request reprint Design, synthesis, and biological evaluation of 1-[(biarylmethyl)methylamino]-2-(2,4-difluorophenyl)-3-(1H-1,2,4-triazol-1-yl)propan-2-ols as potent antifungal agents: new insights into structure-activity relationships
    Rémi Guillon
    Universite de Nantes, Nantes Atlantique Universites, Departement de Pharmacochimie, Cibles et Médicaments des Infections de l Immunité et du Cancer, IICIMED EA 1155, UFR Sciences Pharmaceutiques, 1 rue Gaston Veil, Nantes 44035 Cedex 1, France
    ChemMedChem 6:1806-15. 2011
    ..Therefore, structure-activity relationship studies such as these reveal new insights for the development of future antifungal therapies...
  5. doi request reprint 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
    Rémi Guillon
    Universite de Nantes, Nantes Atlantique Universites, Departement de Pharmacochimie, Cibles et Médicaments des Infections, de l Immunité et du Cancer, IICIMED EA 1155, UFR Sciences Pharmaceutiques, 1 rue Gaston Veil, Nantes F 44035 Cedex 1, France
    Bioorg Med Chem Lett 19:5833-6. 2009
    ..Now we have identified a series of 1-[(1H-indol-5-ylmethyl)amino] derivatives which exhibited potent MICs (<65 ng mL(-1)) against C. albicans strain. The synthesis and SAR behind the indole scaffold will be discussed...
  6. doi request reprint Synthesis and in vitro antifungal evaluation of 2-(2,4-difluorophenyl)-1-[(1H-indol-3-ylmethyl)methylamino]-3-(1H-1,2,4-triazol-1-yl)propan-2-ols
    Rémi Guillon
    Universite de Nantes, Nantes Atlantique Universites, Departement de Pharmacochimie, Cibles et Médicaments des Infections, de l Immunité et du Cancer, IICIMED EA 1155, UFR Sciences Pharmaceutiques, Nantes, France
    J Enzyme Inhib Med Chem 26:261-9. 2011
    ..0 to 381.0 ng/mL) suggesting an inhibition of 14α-demethylase by sterol analysis studies, but are weaker inhibitors compared to their indol-5-ylmethylamino analogs...
  7. doi request reprint 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
    Francis Giraud
    Universite de Nantes, Nantes Atlantique Universites, Departement de Pharmacochimie, Cibles et Médicaments des Infections, de l Immunité et du Cancer, IICIMED EA 1155, UFR de Sciences Pharmaceutiques, 1 rue Gaston Veil, Nantes F 44035 Cedex 1, France
    Bioorg Med Chem Lett 19:301-4. 2009
    ..0 to 23.0ngmL(-1) on Candidaalbicans. These results confirmed both the importance of pi-pi stacking and hydrogen bonding interactions in the active site of CYP51-C. albicans...
  8. doi request reprint Design, synthesis and evaluation of 3-(imidazol- 1-ylmethyl)indoles as antileishmanial agents. Part II
    Francis Giraud
    Departement de Pharmacochimie, Cibles et Médicaments des Infections, de l Immunité et du Cancer, IICIMED EA 1155, UFR de Sciences Pharmaceutiques, Universite de Nantes, Nantes F 44000, France
    J Enzyme Inhib Med Chem 24:1067-75. 2009
    ..Synthesis and biological evaluation of ten new compounds (IC(50) between 2.5 and 5.4 microM) confirmed that only the hydrophobic field is essential for a high level of activity...
  9. doi request reprint Synthesis of new pyridazino[4,5-b]indol-4-ones and pyridazin-3(2H)-one analogs as DYRK1A inhibitors
    Amélie Bruel
    Universite de Nantes, Nantes Atlantique Universites, Laboratoire de Chimie Therapeutique, Cibles et Médicaments des Infections et du Cancer, IICIMED EA 1155, UFR Sciences Pharmaceutiques, 1 rue Gaston Veil, Nantes F 44035 Cedex 1, France
    Bioorg Med Chem Lett 24:5037-40. 2014
    ..In addition, compound 10 exhibited antiproliferative activities in the Huh-7, Caco2 and MDA-MB-231 cell lines. ..
  10. doi request reprint Synthesis and biological evaluation of new 5-benzylated 4-oxo-3,4-dihydro-5H-pyridazino[4,5-b]indoles as PI3Kα inhibitors
    Amélie Bruel
    Universite de Nantes, Nantes Atlantique Universites, Laboratoire de Chimie Therapeutique, Cibles et Médicaments des Infections et du Cancer, IICIMED EA 1155, UFR Sciences Pharmaceutiques, 1 rue Gaston Veil, Nantes F 44035 Cedex 1, France
    Eur J Med Chem 57:225-33. 2012
    ..091 μM. This series exhibited also significant anti-proliferative effects in various human cancer cell lines including those resulting in activation of the PI3K pathway...
  11. doi request reprint Screening for amino acid substitutions in the Candida albicans Erg11 protein of azole-susceptible and azole-resistant clinical isolates: new substitutions and a review of the literature
    Florent Morio
    Universite de Nantes, Nantes Atlantique Universites, Département de Parasitologie et Mycologie Médicale, EA 1155 IICiMed, Faculte de Pharmacie, 1 rue Gaston Veil, 44035 Nantes, France
    Diagn Microbiol Infect Dis 66:373-84. 2010
    ..We suggest that the high genetic polymorphism of ERG11 must be considered in the rationale design of new azole compounds targeting lanosterol 14alpha-demethylase. A review of all Erg11 amino acid polymorphisms described to date is given...
  12. doi request reprint 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
    Julien Defaux
    Universite de Nantes, Nantes Atlantique Universites, Laboratoire de Chimie Therapeutique, Cibles et Médicaments des Infections et du Cancer IICiMed EA 1155, UFR des Sciences Pharmaceutiques et Biologiques, 1 rue Gaston Veil, 44035 Nantes, France
    Bioorg Med Chem Lett 24:3748-52. 2014
    ..Synthesis, structure activity relationship and docking study are reported. In vitro ADME properties and safety data are also discussed. ..
  13. ncbi request reprint Design, synthesis and evaluation of new 6-substituted-5-benzyloxy-4-oxo-4H-pyran-2-carboxamides as potential Src inhibitors
    Julien Farard
    Departement de Pharmacochimie, Faculte de Pharmacie, Universite de Nantes, Nantes Atlantique Universites, Nantes, France
    J Enzyme Inhib Med Chem 23:629-40. 2008
    ..The synthesis of these derivatives and the preliminary results of biological activity will be discussed...
  14. doi request reprint Design, synthesis, and evaluation of 1-(N-benzylamino)-2-phenyl-3-(1H-1,2,4-triazol-1-yl)propan-2-ols as antifungal agents
    Francis Giraud
    Universite de Nantes, Nantes Atlantique Universites, Departement de Pharmacochimie, Biomolécules et Cibles Thérapeutiques, BioCiT EA 1155, UFR de Sciences Pharmaceutiques, 1 rue Gaston Veil, Nantes, F 44035 Cedex 1, France
    Bioorg Med Chem Lett 18:1820-4. 2008
    ..The most active compound 7b was docked into a home-made 3D model of the targeted enzyme confirming the importance of Tyr118, His377, and Ser378 residues in its binding mode...