Sebastien Fortin

Summary

Country: Canada

Publications

  1. ncbi Synthesis, antiproliferative activity evaluation and structure-activity relationships of novel aromatic urea and amide analogues of N-phenyl-N'-(2-chloroethyl)ureas
    Sebastien Fortin
    Unité des Biotechnologies et de Bioingénierie, Centre de Recherche, C H U Q, Hopital Saint Francois d Assise, Quebec G1L 3L5, Canada
    Eur J Med Chem 45:2928-37. 2010
  2. ncbi Quick and simple detection technique to assess the binding of antimicrotubule agents to the colchicine-binding site
    Sebastien Fortin
    Unité des Biotechnologies et de Bioingénierie, Centre de Recherche, C, H, U, Q, Hopital Saint Francois d Assise, Quebec, QC, G1L 3L5, Canada
    Biol Proced Online 12:113-7. 2010
  3. ncbi Characterization of the covalent binding of N-phenyl-N'-(2-chloroethyl)ureas to {beta}-tubulin: importance of Glu198 in microtubule stability
    Sebastien Fortin
    Unité des Biotechnologies et de Bioingénierie, Centre de Recherche, Centre Hospitalier Universitaire de Quebec, Hopital Saint Francois d Assise, 10 rue de l Espinay, Quebec, Canada
    J Pharmacol Exp Ther 336:460-7. 2011
  4. ncbi Substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonamides as antimitotics. Antiproliferative, antiangiogenic and antitumoral activity, and quantitative structure-activity relationships
    Sebastien Fortin
    Unité des Biotechnologies et de Bioingénierie, Centre de Recherche, CHUQ, Hopital Saint Francois d Assise, Quebec, QC, Canada
    Eur J Med Chem 46:5327-42. 2011
  5. ncbi Mechanism of action of N-phenyl-N'-(2-chloroethyl)ureas in the colchicine-binding site at the interface between alpha- and beta-tubulin
    Sebastien Fortin
    Unité des Biotechnologies et de Bioingénierie, Centre de Recherche, C H U Q, Hopital Saint Francois d Assise, Universite Laval, Quebec, Canada G1L 3L5
    Bioorg Med Chem 17:3690-7. 2009
  6. ncbi A comparative molecular field and comparative molecular similarity indices analyses (CoMFA and CoMSIA) of N-phenyl-N'-(2-chloroethyl)ureas targeting the colchicine-binding site as anticancer agents
    Sebastien Fortin
    Unité des Biotechnologies et de Bioingénierie, Centre de Recherche, C H U Q, Hopital Saint Francois d Assise, Universite Laval, Quebec, Que, Canada G1L 3L5
    Bioorg Med Chem 16:1914-26. 2008
  7. ncbi Design, synthesis, biological evaluation, and structure-activity relationships of substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonates as new tubulin inhibitors mimicking combretastatin A-4
    Sebastien Fortin
    Unité des Biotechnologies et de Bioingénierie, Centre de Recherche, CHUQ, Hôpital Saint François d Assise, Québec, Québec, Canada
    J Med Chem 54:4559-80. 2011
  8. ncbi N-Phenyl-N'-(2-chloroethyl)urea analogues of combretastatin A-4: Is the N-phenyl-N'-(2-chloroethyl)urea pharmacophore mimicking the trimethoxy phenyl moiety?
    Sebastien Fortin
    Unité des Biotechnologies et de Bioingénierie, Centre de Recherche, C H U Q, Hopital Saint Francois d Assise, Universite Laval, Que, Canada G1L 3L5
    Bioorg Med Chem Lett 17:2000-4. 2007
  9. ncbi Synthesis, biological evaluation, and structure-activity relationships of novel substituted N-phenyl ureidobenzenesulfonate derivatives blocking cell cycle progression in S-phase and inducing DNA double-strand breaks
    Vanessa Turcotte
    Unité des Biotechnologies et de Bioingénierie, Centre de Recherche, C H U Q, Hopital Saint Francois d Assise, Quebec, QC, G1L 3L5, Canada
    J Med Chem 55:6194-208. 2012
  10. ncbi N-Phenyl-N'-(2-chloroethyl)ureas (CEU) as potential antineoplastic agents. Part 2: role of omega-hydroxyl group in the covalent binding to beta-tubulin
    Sebastien Fortin
    Unité des Biotechnologies et de Bioingénierie, Centre de Recherche, C H U Q, Hopital Saint Francois d Assise, Universite Laval, Quebec, QC, Canada G01L 3L5
    Bioorg Med Chem 15:1430-8. 2007

Collaborators

Detail Information

Publications14

  1. ncbi Synthesis, antiproliferative activity evaluation and structure-activity relationships of novel aromatic urea and amide analogues of N-phenyl-N'-(2-chloroethyl)ureas
    Sebastien Fortin
    Unité des Biotechnologies et de Bioingénierie, Centre de Recherche, C H U Q, Hopital Saint Francois d Assise, Quebec G1L 3L5, Canada
    Eur J Med Chem 45:2928-37. 2010
    ..4 to 25 microM. CAU, CA, CPA and Acr exhibited interesting antiproliferative activity through mechanism(s) of action unrelated to the acylation of glutamic acid at position 198 on beta-tubulin that is characterizing CEU...
  2. ncbi Quick and simple detection technique to assess the binding of antimicrotubule agents to the colchicine-binding site
    Sebastien Fortin
    Unité des Biotechnologies et de Bioingénierie, Centre de Recherche, C, H, U, Q, Hopital Saint Francois d Assise, Quebec, QC, G1L 3L5, Canada
    Biol Proced Online 12:113-7. 2010
    ..The occupancy of colchicine-binding site by pertinent antimitotics inhibits the formation of the EBI: β-tubulin adduct, resulting in an assay that allows the screening of new molecules targeting this binding site...
  3. ncbi Characterization of the covalent binding of N-phenyl-N'-(2-chloroethyl)ureas to {beta}-tubulin: importance of Glu198 in microtubule stability
    Sebastien Fortin
    Unité des Biotechnologies et de Bioingénierie, Centre de Recherche, Centre Hospitalier Universitaire de Quebec, Hopital Saint Francois d Assise, 10 rue de l Espinay, Quebec, Canada
    J Pharmacol Exp Ther 336:460-7. 2011
    ....
  4. ncbi Substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonamides as antimitotics. Antiproliferative, antiangiogenic and antitumoral activity, and quantitative structure-activity relationships
    Sebastien Fortin
    Unité des Biotechnologies et de Bioingénierie, Centre de Recherche, CHUQ, Hopital Saint Francois d Assise, Quebec, QC, Canada
    Eur J Med Chem 46:5327-42. 2011
    ....
  5. ncbi Mechanism of action of N-phenyl-N'-(2-chloroethyl)ureas in the colchicine-binding site at the interface between alpha- and beta-tubulin
    Sebastien Fortin
    Unité des Biotechnologies et de Bioingénierie, Centre de Recherche, C H U Q, Hopital Saint Francois d Assise, Universite Laval, Quebec, Canada G1L 3L5
    Bioorg Med Chem 17:3690-7. 2009
    ..Of interest, in vivo acylation of acidic amino acid residues by xenobiotics is an unusual reaction and may open new approaches for the design of irreversible protein inhibitors such as tubulin...
  6. ncbi A comparative molecular field and comparative molecular similarity indices analyses (CoMFA and CoMSIA) of N-phenyl-N'-(2-chloroethyl)ureas targeting the colchicine-binding site as anticancer agents
    Sebastien Fortin
    Unité des Biotechnologies et de Bioingénierie, Centre de Recherche, C H U Q, Hopital Saint Francois d Assise, Universite Laval, Quebec, Que, Canada G1L 3L5
    Bioorg Med Chem 16:1914-26. 2008
    ..These models will inspire the design of new CEU derivatives with enhanced inhibition of tumor cell growth and targeting specificity of beta(II)-tubulin and the cytoskeleton...
  7. ncbi Design, synthesis, biological evaluation, and structure-activity relationships of substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonates as new tubulin inhibitors mimicking combretastatin A-4
    Sebastien Fortin
    Unité des Biotechnologies et de Bioingénierie, Centre de Recherche, CHUQ, Hôpital Saint François d Assise, Québec, Québec, Canada
    J Med Chem 54:4559-80. 2011
    ..PIB-SOs were subjected to CoMFA and CoMSIA analyses to establish quantitative structure-activity relationships...
  8. ncbi N-Phenyl-N'-(2-chloroethyl)urea analogues of combretastatin A-4: Is the N-phenyl-N'-(2-chloroethyl)urea pharmacophore mimicking the trimethoxy phenyl moiety?
    Sebastien Fortin
    Unité des Biotechnologies et de Bioingénierie, Centre de Recherche, C H U Q, Hopital Saint Francois d Assise, Universite Laval, Que, Canada G1L 3L5
    Bioorg Med Chem Lett 17:2000-4. 2007
    ..Covalent binding of 2a, 3a, and 3b to the colchicine-binding site of beta-tubulin was confirmed also using SDS-PAGE and competition assays...
  9. ncbi Synthesis, biological evaluation, and structure-activity relationships of novel substituted N-phenyl ureidobenzenesulfonate derivatives blocking cell cycle progression in S-phase and inducing DNA double-strand breaks
    Vanessa Turcotte
    Unité des Biotechnologies et de Bioingénierie, Centre de Recherche, C H U Q, Hopital Saint Francois d Assise, Quebec, QC, G1L 3L5, Canada
    J Med Chem 55:6194-208. 2012
    ..These new compounds are members of a promising new class of anticancer agents...
  10. ncbi N-Phenyl-N'-(2-chloroethyl)ureas (CEU) as potential antineoplastic agents. Part 2: role of omega-hydroxyl group in the covalent binding to beta-tubulin
    Sebastien Fortin
    Unité des Biotechnologies et de Bioingénierie, Centre de Recherche, C H U Q, Hopital Saint Francois d Assise, Universite Laval, Quebec, QC, Canada G01L 3L5
    Bioorg Med Chem 15:1430-8. 2007
    ..We have confirmed that the pentyl substituted CEUs 1f, 2f, and 3e are still covalently binding to beta-tubulin and still arrest cell division in G(2)/M phase...
  11. ncbi A comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA) of anthranilamide derivatives that are multidrug resistance modulators
    Philippe Labrie
    Unité des Biotechnologies et de Bioingénierie, Hopital Saint Francois d Assise, Quebec City, Quebec G1L 3L5, Canada
    J Med Chem 49:7646-60. 2006
    ..These most comprehensive CoMFA and CoMSIA models are useful in understanding the structure-activity relationships of anthranilamide derivatives as well as aid in the design of novel derivatives with enhanced modulation of P-gp activity...
  12. ncbi Optimized N-phenyl-N'-(2-chloroethyl)ureas as potential antineoplastic agents: synthesis and growth inhibition activity
    Emmanuel Moreau
    Unité de Biotechnologie et de Bioingénierie, C H U Q, Hopital Saint Francois d Assise, Universite Laval, Quebec, QC, Canada G1L 3L5
    Bioorg Med Chem 13:6703-12. 2005
    ..They are more potent by approximately an order of magnitude than previously described CEU analogues. As such, they are attractive hit compounds for the development of potent new alkylating antitubulin drugs...
  13. ncbi Inhibitory effects of cytoskeleton disrupting drugs and GDP-locked Rab mutants on bradykinin B2 receptor cycling
    Xavier Charest-Morin
    Centre de Recherche en Rhumatologie et Immunologie, Centre Hospitalier Universitaire de Quebec, Quebec QC, Canada, G1V 4G2
    Pharmacol Res 71:44-52. 2013
    ..However, tubulin ligands do not suppress the tested desensitization or resensitization mechanisms of the B2R...
  14. ncbi Effects of inactivation-resistant agonists on the signalling, desensitization and down-regulation of bradykinin B(2) receptors
    Marie Thérèse Bawolak
    Centre de Recherche en Rhumatologie et Immunologie, Centre Hospitalier Universitaire de Québec and Department of Medicine, Universite Laval, Quebec, QC, Canada
    Br J Pharmacol 158:1375-86. 2009
    ..Further, B-9972 and compound 47a, unlike BK, efficiently down-regulated BK B(2) receptors...