Search Results - "Ferland, Jean Marie"
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Olefin ring-closing metathesis as a powerful tool in drug discovery and development – potent macrocyclic inhibitors of the hepatitis C virus NS3 protease
Published in Journal of organometallic chemistry (01-12-2006)“…Tripeptide dienes composed of three unnatural amino acid residues with numerous chiral centers were efficiently converted to macrocyclic peptides, in high…”
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Binding Mode Determination of Benzimidazole Inhibitors of the Hepatitis C Virus RNA Polymerase by a Structure and Dynamics Strategy
Published in Angewandte Chemie International Edition (20-08-2004)“…A novel strategy involving NMR, medicinal chemistry, and molecular modeling is described for determining the binding mode of ligands and the binding roles of…”
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Synthesis of BILN 2061, an HCV NS3 Protease Inhibitor with Proven Antiviral Effect in Humans
Published in Organic letters (19-08-2004)“…The synthesis of BILN 2061, an NS3 protease inhibitor with proven antiviral effect in humans, was accomplished in a convergent manner from four building…”
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RCM of Tripeptide Dienes Containing a Chiral Vinylcyclopropane Moiety: Impact of Different Ru-Based Catalysts on the Stereochemical Integrity of the Macrocyclic Products
Published in Journal of organic chemistry (23-12-2005)“…Tripeptide dienes containing an (1R,2S)-vinyl aminocyclopropylcarboxylate residue were cyclized to β-strand scaffolds under ring-closing metathesis (RCM)…”
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Potent Inhibitors of the Hepatitis C Virus NS3 Protease: Design and Synthesis of Macrocyclic Substrate-Based β-Strand Mimics
Published in Journal of organic chemistry (17-09-2004)“…The virally encoded NS3 protease is essential to the life cycle of the hepatitis C virus (HCV), an important human pathogen causing chronic hepatitis,…”
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Peptidomimetic Inhibitors of Herpes Simplex Virus Ribonucleotide Reductase with Improved in Vivo Antiviral Activity
Published in Journal of medicinal chemistry (11-10-1996)“…We have been investigating the potential of a new class of antiviral compounds. These peptidomimetic derivatives prevent association of the two subunits of…”
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Binding Mode Determination of Benzimidazole Inhibitors of the Hepatitis C Virus RNA Polymerase by a Structure and Dynamics Strategy
Published in Angewandte Chemie (20-08-2004)“…Eine neuartige Strategie, die NMR‐Spektroskopie, medizinische Chemie und Molecular Modeling umfasst, diente zur Bestimmung der Bindungsweise von Liganden und…”
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Peptidomimetic inhibitors of herpes simplex virus ribonucleotide reductase: a new class of antiviral agents
Published in Journal of medicinal chemistry (01-09-1995)“…We have been investigating a new class of antiviral compounds effective against herpes simplex virus (HSV) in vitro and in vivo. Antiviral activity results…”
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Ureido-Based Peptidomimetic Inhibitors of Herpes Simplex Virus Ribonucleotide Reductase: An Investigation of Inhibitor Bioactive Conformation
Published in Journal of medicinal chemistry (24-05-1996)“…We have been investigating peptidomimetic inhibitors of herpes simplex virus (HSV) ribonucleotide reductase (RR). These inhibitors bind to the HSV RR large…”
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Structure−Activity Study on a Novel Series of Macrocyclic Inhibitors of the Hepatitis C Virus NS3 Protease Leading to the Discovery of BILN 2061
Published in Journal of medicinal chemistry (25-03-2004)“…From the discovery of competitive hexapeptide inhibitors, potent and selective HCV NS3 protease macrocyclic inhibitors have been identified. Structure−activity…”
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Herpes simplex virus ribonucleotide reductase subunit association inhibitors: the effect and conformation of beta-alkylated aspartic acid derivatives
Published in Bioorganic & medicinal chemistry (01-09-1994)“…Incorporating beta-alkylated aspartic acid derivatives into herpes simplex virus ribonucleotide reductase subunit association inhibitors can improve inhibitor…”
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Potent Inhibitors of the Hepatitis C Virus NS3 Protease: Design and Synthesis of Macrocyclic Substrate-Based [beta]-Strand Mimics
Published in Journal of organic chemistry (30-06-2008)“…The virally encoded NS3 protease is essential to the life cycle of the hepatitis C virus (HCV), an important human pathogen causing chronic hepatitis,…”
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Nonpeptidic, Monocharged, Cell Permeable Ligands for the p56lck SH2 Domain
Published in Journal of medicinal chemistry (19-07-2001)“…p56lck is a member of the src family of tyrosine kinases and plays a critical role in the signal transduction events that lead to T cell activation. Ligands…”
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Nonpeptidic, monocharged, cell permeable ligands for the p561ck SH2 domain
Published in Journal of medicinal chemistry (2001)Get full text
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Ligands for the Tyrosine Kinase p56 lck SH2 Domain: Discovery of Potent Dipeptide Derivatives with Monocharged, Nonhydrolyzable Phosphate Replacements
Published in Journal of medicinal chemistry (20-05-1999)“…p56 lck is a member of the src family of tyrosine kinases. Through modular binding units called SH2 domains, p56 lck promotes phosphotyrosine-dependent…”
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Phosphotyrosine-Containing Dipeptides as High-Affinity Ligands for the p56 lck SH2 Domain
Published in Journal of medicinal chemistry (25-02-1999)“…Src homology-2 (SH2) domains are noncatalytic motifs containing approximately 100 amino acid residues that are involved in intracellular signal transduction…”
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Phosphotyrosine-Containing Dipeptides as High-Affinity Ligands for the p56lck SH2 Domain
Published in Journal of medicinal chemistry (25-02-1999)“…Src homology-2 (SH2) domains are noncatalytic motifs containing approximately 100 amino acid residues that are involved in intracellular signal transduction…”
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Ligands for the Tyrosine Kinase p56lck SH2 Domain: Discovery of Potent Dipeptide Derivatives with Monocharged, Nonhydrolyzable Phosphate Replacements
Published in Journal of medicinal chemistry (20-05-1999)“…p56lck is a member of the src family of tyrosine kinases. Through modular binding units called SH2 domains, p56lck promotes phosphotyrosine-dependent…”
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