Christophe Biot

Summary

Country: France

Publications

  1. pmc Assessment of Plasmodium falciparum resistance to ferroquine (SSR97193) in field isolates and in W2 strain under pressure
    Wassim Daher
    INSERM U547, Institut Pasteur, 1 rue du Pr Calmette, BP 245, 59019 Lille, France
    Malar J 5:11. 2006
  2. ncbi request reprint Probing the role of the covalent linkage of ferrocene into a chloroquine template
    Christophe Biot
    Unite de Catalyse et Chimie du Solide UMR CNRS 8181, ENSCL, Batiment C7, USTL, B P 90108, 59652, Villeneuve d Ascq Cedex, France
    J Med Chem 49:4707-14. 2006
  3. ncbi request reprint Design, synthesis, and antimalarial activity of structural chimeras of thiosemicarbazone and ferroquine analogues
    Christophe Biot
    Université des Sciences et Technologies, Unité de Catalyse et de Chimie du Solide UMR CNRS 8181, ENSCL, Batiment C7, BP 90108, 59652 Villeneuve d Ascq cedex, France
    Bioorg Med Chem Lett 17:6434-8. 2007
  4. ncbi request reprint Novel approaches to antimalarial drug discovery
    Christophe Biot
    Unite de Catalyse et Chimie du Solide UMR CNRS 8181, ENSCL, Batiment C7, USTL B P 90108, 59652, Villeneuve d Ascq Cedex, France
    Infect Disord Drug Targets 6:173-204. 2006
  5. ncbi request reprint 5-substituted tetrazoles as bioisosteres of carboxylic acids. Bioisosterism and mechanistic studies on glutathione reductase inhibitors as antimalarials
    Christophe Biot
    Bioinformatique génomique et structurale, CP 165 61, Universite Libre de Bruxelles, 50 Av F D Roosevelt, B 1050 Brussels, Belgium
    J Med Chem 47:5972-83. 2004
  6. ncbi request reprint Design and synthesis of hydroxyferroquine derivatives with antimalarial and antiviral activities
    Christophe Biot
    Unite de Catalyse et Chimie du Solide UMR CNRS 8181, ENSCL, Batiment C7, USTL, B P 90108, 59652 Villeneuve d Ascq cedex, France
    J Med Chem 49:2845-9. 2006
  7. doi request reprint The ferroquine antimalarial conundrum: redox activation and reinvasion inhibition
    Faustine Dubar
    Université Lille1, Unite de Catalyse et Chimie du Solide UMR CNRS 8181, B P 90108, 59652 Villeneuve d Ascq cedex, France
    Angew Chem Int Ed Engl 52:7690-3. 2013
  8. doi request reprint The antimalarial ferroquine: role of the metal and intramolecular hydrogen bond in activity and resistance
    Faustine Dubar
    Université de Lille, Unité de Catalyse et Chimie du Solide UMR CNRS, ENSCL, Villeneuve d Ascq, France
    ACS Chem Biol 6:275-87. 2011
  9. doi request reprint Enhancement of the antimalarial activity of ciprofloxacin using a double prodrug/bioorganometallic approach
    Faustine Dubar
    Universite de Lille 1, CNRS UMR 8181, ENSCL, Villeneuve d Ascq Cedex, France
    J Med Chem 52:7954-7. 2009
  10. doi request reprint Ferroquine, an ingenious antimalarial drug: thoughts on the mechanism of action
    Faustine Dubar
    Universite des Sciences et Technologies de Lille, Unité de Catalyse et Chimie du Solide, UMR CNRS 8181, Ecole Nationale Superieure de Chimie de Lille, Batiment C7, Villeneuve d Ascq Cedex, France
    Molecules 13:2900-7. 2008

Collaborators

Detail Information

Publications20

  1. pmc Assessment of Plasmodium falciparum resistance to ferroquine (SSR97193) in field isolates and in W2 strain under pressure
    Wassim Daher
    INSERM U547, Institut Pasteur, 1 rue du Pr Calmette, BP 245, 59019 Lille, France
    Malar J 5:11. 2006
    ..FQ is also curative on rodent malaria parasites. As FQ will be tested in patients, the potential for resistance to this drug was evaluated...
  2. ncbi request reprint Probing the role of the covalent linkage of ferrocene into a chloroquine template
    Christophe Biot
    Unite de Catalyse et Chimie du Solide UMR CNRS 8181, ENSCL, Batiment C7, USTL, B P 90108, 59652, Villeneuve d Ascq Cedex, France
    J Med Chem 49:4707-14. 2006
    ..Current data reinforced our choice of FQ as a drug candidate...
  3. ncbi request reprint Design, synthesis, and antimalarial activity of structural chimeras of thiosemicarbazone and ferroquine analogues
    Christophe Biot
    Université des Sciences et Technologies, Unité de Catalyse et de Chimie du Solide UMR CNRS 8181, ENSCL, Batiment C7, BP 90108, 59652 Villeneuve d Ascq cedex, France
    Bioorg Med Chem Lett 17:6434-8. 2007
    ..The presence of the aminoquinoline structure, allowing transport of the compounds to the food vacuole of the parasite, seems to be the major contributor to antimalarial activity...
  4. ncbi request reprint Novel approaches to antimalarial drug discovery
    Christophe Biot
    Unite de Catalyse et Chimie du Solide UMR CNRS 8181, ENSCL, Batiment C7, USTL B P 90108, 59652, Villeneuve d Ascq Cedex, France
    Infect Disord Drug Targets 6:173-204. 2006
    ....
  5. ncbi request reprint 5-substituted tetrazoles as bioisosteres of carboxylic acids. Bioisosterism and mechanistic studies on glutathione reductase inhibitors as antimalarials
    Christophe Biot
    Bioinformatique génomique et structurale, CP 165 61, Universite Libre de Bruxelles, 50 Av F D Roosevelt, B 1050 Brussels, Belgium
    J Med Chem 47:5972-83. 2004
    ..The potential binding site of these molecules is discussed in light of the recently solved crystallographic structure of P. falciparum enzyme...
  6. ncbi request reprint Design and synthesis of hydroxyferroquine derivatives with antimalarial and antiviral activities
    Christophe Biot
    Unite de Catalyse et Chimie du Solide UMR CNRS 8181, ENSCL, Batiment C7, USTL, B P 90108, 59652 Villeneuve d Ascq cedex, France
    J Med Chem 49:2845-9. 2006
    ..These new drugs may offer an interesting alternative for Asia where SARS originated and malaria has remained endemic...
  7. doi request reprint The ferroquine antimalarial conundrum: redox activation and reinvasion inhibition
    Faustine Dubar
    Université Lille1, Unite de Catalyse et Chimie du Solide UMR CNRS 8181, B P 90108, 59652 Villeneuve d Ascq cedex, France
    Angew Chem Int Ed Engl 52:7690-3. 2013
    ..It is based on the production of HO(·) in the acidic and oxidizing environment of the digestive vacuole of the malaria parasite and implies that, with ferroquine, reinvasion can be inhibited...
  8. doi request reprint The antimalarial ferroquine: role of the metal and intramolecular hydrogen bond in activity and resistance
    Faustine Dubar
    Université de Lille, Unité de Catalyse et Chimie du Solide UMR CNRS, ENSCL, Villeneuve d Ascq, France
    ACS Chem Biol 6:275-87. 2011
    ..Ultrastructural studies revealed that FQ and Me-FQ but not RQ or Me-RQ break down the parasite digestive vacuole membrane, which could be related to the ability of the former to generate hydroxyl radicals...
  9. doi request reprint Enhancement of the antimalarial activity of ciprofloxacin using a double prodrug/bioorganometallic approach
    Faustine Dubar
    Universite de Lille 1, CNRS UMR 8181, ENSCL, Villeneuve d Ascq Cedex, France
    J Med Chem 52:7954-7. 2009
    ..These achiral derivatives killed parasites more rapidly than did ciprofloxacin. Compounds 2 and 4 were revealed to be promising leads, creating a new family of antimalarial agents...
  10. doi request reprint Ferroquine, an ingenious antimalarial drug: thoughts on the mechanism of action
    Faustine Dubar
    Universite des Sciences et Technologies de Lille, Unité de Catalyse et Chimie du Solide, UMR CNRS 8181, Ecole Nationale Superieure de Chimie de Lille, Batiment C7, Villeneuve d Ascq Cedex, France
    Molecules 13:2900-7. 2008
    ..After fifteen years of effort, it is now possible to propose a multifactorial mechanism of action of FQ by its capacity to target lipids, to inhibit the formation of hemozoin and to generate reactive oxygen species...
  11. doi request reprint Antimalarial activities of ferroquine conjugates with either glutathione reductase inhibitors or glutathione depletors via a hydrolyzable amide linker
    Natascha Chavain
    Universite de Lille 1, Unite de Catalyse et Chimie du Solide UMR CNRS 8181, ENSCL, Batiment C7, B P 90108, 59652 Villeneuve d Ascq cedex, France
    Bioorg Med Chem 17:8048-59. 2009
    ....
  12. doi request reprint In situ nanochemical imaging of label-free drugs: a case study of antimalarials in Plasmodium falciparum-infected erythrocytes
    Faustine Dubar
    Universite Lille Nord de France, Université Lille1, UCCS UMR CNRS 8181, 59652 Villeneuve d Ascq cedex, France
    Chem Commun (Camb) 48:910-2. 2012
    ..Our approach may be applied to a wide range of domains where quantitative chemical imaging of drugs at the sub-cellular level appears critical...
  13. doi request reprint Investigation of the redox behavior of ferroquine, a new antimalarial
    Natascha Chavain
    Universite des Sciences et Technologies de Lille, Unite de Catalyse et Chimie du Solide UMR CNRS 8181, Ecole Nationale Superieure de Chimie de Lille, Batiment C7, B P 90108, 59652 Villeneuve d Ascq cedex, France
    Mol Pharm 5:710-6. 2008
    ....
  14. ncbi request reprint Insights into the mechanism of action of ferroquine. Relationship between physicochemical properties and antiplasmodial activity
    Christophe Biot
    Laboratoire de Catalyse de Lille UMR CNRS 8010, ENSCL, Batiment C7, Université des Sciences et Technologies, B P 90108, 59652, Villeneuve d Ascq Cedex, France
    Mol Pharm 2:185-93. 2005
    ..Increased lipophilicity, differences in geometric and electronic structure, and changes in the N-N distances in FQ compared to CQ probably explain its activity against CQ-resistant parasites...
  15. ncbi request reprint Free-energy calculations of protein-ligand cation-pi and amino-pi interactions: from vacuum to proteinlike environments
    Christophe Biot
    Ingénierie Biomoléculaire, Universite Libre de Bruxelles, CP 165 64, 50 Avenue Roosevelt, B 1050 Brussels, Belgium
    J Am Chem Soc 125:13988-94. 2003
    ..Remarkably, these free-energy values of cation/amino-pi interactions correlate well with their frequency of occurrences in protein-ligand structures, which corroborates our approach in the absence of experimental data...
  16. ncbi request reprint Probing the energetic and structural role of amino acid/nucleobase cation-pi interactions in protein-ligand complexes
    Christophe Biot
    Ingénierie Biomoléculaire, Universite Libre de Bruxelles, CP 165 64, 50 Avenue F D Roosevelt, B 1050 Brussels, Belgium
    J Biol Chem 277:40816-22. 2002
    ..The systematic association of these motifs with specific ligand molecules in unrelated protein sequences raises the question of their role in protein-ligand structure, stability, and recognition...
  17. ncbi request reprint In vitro metabolism of ferroquine (SSR97193) in animal and human hepatic models and antimalarial activity of major metabolites on Plasmodium falciparum
    Wassim Daher
    INSERM U547, Institut Pasteur, 1 rue du Professeur P Calmette, B P 245, 59019 Lille Cedex, France
    Drug Metab Dispos 34:667-82. 2006
    ..These results further support the potential use of ferroquine against human malaria...
  18. ncbi request reprint Ferrocene conjugates of chloroquine and other antimalarials: the development of ferroquine, a new antimalarial
    Daniel Dive
    INSERM U547, Institut Pasteur, 1 rue du Pr Calmette, B P 245, 59019 Lille Cedex, France
    ChemMedChem 3:383-91. 2008
  19. ncbi request reprint Double-drug development against antioxidant enzymes from Plasmodium falciparum
    Christophe Biot
    UMR 8525 CNRS Université de Lille 2, Institut de Biologie de Lille, Lille, France
    Redox Rep 8:280-3. 2003
    ..falciparum, future development of antimalarial drug-candidates that act by perturbing the redox equilibrium of parasites is based on the design of new double-drugs based on TrxR inhibitors as potential antimalarial drug candidates...
  20. ncbi request reprint Synthesis of ferroquine enantiomers: first investigation of effects of metallocenic chirality upon antimalarial activity and cytotoxicity
    Laurence Delhaes
    INSERM U 42, 369 rue Jules Guesde BP 39, 59651 Villeneuve d Ascq Cedex, France
    Chembiochem 3:418-23. 2002
    ..Actually, the racemate represents the optimal formulation. To the best of our knowledge, this is the first investigation of biological activities of compounds with metallocenic chirality...