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Designing heterocyclic selective kinase inhibitors: from concept to new drug candidates

ARKIVOC, 2006-04, Vol.2006 (7), p.496-508

2006

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Design and Synthesis of the First Generation of Novel Potent, Selective, and in Vivo Active (Benzothiazol-2-yl)acetonitrile Inhibitors of the c-Jun N-Terminal Kinase

Journal of medicinal chemistry, 2005-07, Vol.48 (14), p.4596-4607

2005

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Signal Transduction: An Exciting Field of Investigation for Small Molecule Drug Discovery

Molecules (Basel, Switzerland), 2003-04, Vol.8 (4), p.349-358

Halazy, Serge

2003

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A Simple One-Pot Preparation of N,N’-Unsymmetrical Ureas from N-Boc Protected Primary Anilines and Amines

Synlett, 1996-06, Vol.1996 (6), p.507-508

1996

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In vitro and in vivo pharmacological profile of AS057278, a selective d -amino acid oxidase inhibitor with potential anti-psychotic properties

European neuropsychopharmacology, 2008-03, Vol.18 (3), p.200-214

2008

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3,6-Dibromocarbazole Piperazine Derivatives of 2-Propanol as First Inhibitors of Cytochrome c Release via Bax Channel Modulation

Journal of medicinal chemistry, 2003-10, Vol.46 (21), p.4365-4368

2003

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Synthesis of arylpiperazines via nucleophilic aromatic substitution of ( η6-fluoroarene)tricarbonylchromium complexes

Tetrahedron letters, 1996-11, Vol.37 (47), p.8487-8488

1996

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Chemical genetics: toward the next generation of molecular medicines

Pharmacogenomics, 2004-10, Vol.5 (7), p.757-761

Halazy, Serge

2004

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(Aryloxy)methylsilane Derivatives as New Cholesterol Biosynthesis Inhibitors: Synthesis and Hypocholesterolemic Activity of a New Class of Squalene Epoxidase Inhibitors

Journal of medicinal chemistry, 1995-08, Vol.38 (17), p.3207-3216

1995

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Synthesis and serotonergic activity of arylpiperazide derivatives of serotonin: potent agonists for 5-HT1D receptors

Journal of medicinal chemistry, 1995-09, Vol.38 (18), p.3602-3607

1995

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Design, Synthesis, and Biological Activity of Novel, Potent, and Selective (Benzoylaminomethyl)thiophene Sulfonamide Inhibitors of c-Jun-N-Terminal Kinase

Journal of medicinal chemistry, 2004-12, Vol.47 (27), p.6921-6934

2004

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GLEPP1/Protein-tyrosine Phosphatase ϕ Inhibitors Block Chemotaxis in Vitro and in Vivo and Improve Murine Ulcerative Colitis

The Journal of biological chemistry, 2009-04, Vol.284 (17), p.11385-11395

2009

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G-protein coupled receptors bivalent ligands and drug design

Expert opinion on therapeutic patents, 1999-04, Vol.9 (4), p.431-446

Halazy, Serge

1999

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Phosphonate derivatives of N9-benzylguanine: a new class of potent purine nucleoside phosphorylase inhibitors

Bioorganic & medicinal chemistry letters, 1992-01, Vol.2 (5), p.407-410

1992

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Studies on the synthesis of the antitumor agent CC-1065. Synthesis of PDE I and PDE II, inhibitors of cyclic adenosine-3',5'-monophosphate phosphodiesterase using the 3,3'-bipyrrole strategy

Journal of the American Chemical Society, 1987-04, Vol.109 (9), p.2711-2717

1987

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Discovery and Development of a New Class of Potent, Selective, Orally Active Oxytocin Receptor Antagonists

Journal of medicinal chemistry, 2005-12, Vol.48 (24), p.7882-7905

2005

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GLEPP1/Protein-tyrosine Phosphatase φ Inhibitors Block Chemotaxis in Vitro and in Vivo and Improve Murine Ulcerative ColitisS

The Journal of biological chemistry, 2009-04, Vol.284 (17), p.11385-11395

2009

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GLEPP1/Protein-tyrosine Phosphatase Ï Inhibitors Block Chemotaxis in Vitro and in Vivo and Improve Murine Ulcerative Colitis

The Journal of biological chemistry, 2009-04, Vol.284 (17), p.11385

2009

Volltextzugriff (PDF)

GLEPP1/Protein-tyrosine Phosphatase {phi} Inhibitors Block Chemotaxis in Vitro and in Vivo and Improve Murine Ulcerative Colitis

The Journal of biological chemistry, 2009, Vol.284 (17), p.11385-11395

2009

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Serotonin dimers: application of the bivalent ligand approach to the design of new potent and selective 5-HT(1B/1D) agonists

Journal of medicinal chemistry, 1996-12, Vol.39 (25), p.4920-4927

1996

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Serotonin Dimers: Application of the Bivalent Ligand Approach to the Design of New Potent and Selective 5-HT1B/1D Agonists

Journal of medicinal chemistry, 1996-12, Vol.39 (25), p.4920-4927

1996

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Differentiation between Partial Agonists and Neutral 5-HT1B Antagonists by Chemical Modulation of 3-[3-(N,N-Dimethylamino)propyl]-4-hydroxy- N-[4-(pyridin-4-yl)phenyl]benzamide (GR-55562)

Journal of medicinal chemistry, 1997-10, Vol.40 (22), p.3542-3550

1997

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Section Review: Cardiovascular & Renal: Squalene epoxidase inhibitors

Expert opinion on therapeutic patents, 1996-11, Vol.6 (11), p.1165-1173

1996

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Dimerization of sumatriptan as an efficient way to design a potent, centrally and orally active 5-HT1B agonist

Bioorganic & medicinal chemistry letters, 1998-03, Vol.8 (6), p.675-680

1998

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F 11356, a novel 5-hydroxytryptamine (5-HT) derivative with potent, selective, and unique high intrinsic activity at 5-HT1B/1D receptors in models relevant to migraine

The Journal of pharmacology and experimental therapeutics, 1999-07, Vol.290 (1), p.83

1999

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Designing heterocyclic selective kinase inhibitors: from concept to new drug candidates

Design and Synthesis of the First Generation of Novel Potent, Selective, and in Vivo Active (Benzothiazol-2-yl)acetonitrile Inhibitors of the c-Jun N-Terminal Kinase

Signal Transduction: An Exciting Field of Investigation for Small Molecule Drug Discovery

A Simple One-Pot Preparation of N,N’-Unsymmetrical Ureas from N-Boc Protected Primary Anilines and Amines

In vitro and in vivo pharmacological profile of AS057278, a selective d -amino acid oxidase inhibitor with potential anti-psychotic properties

3,6-Dibromocarbazole Piperazine Derivatives of 2-Propanol as First Inhibitors of Cytochrome c Release via Bax Channel Modulation

Synthesis of arylpiperazines via nucleophilic aromatic substitution of ( η6-fluoroarene)tricarbonylchromium complexes

Chemical genetics: toward the next generation of molecular medicines

(Aryloxy)methylsilane Derivatives as New Cholesterol Biosynthesis Inhibitors: Synthesis and Hypocholesterolemic Activity of a New Class of Squalene Epoxidase Inhibitors

Synthesis and serotonergic activity of arylpiperazide derivatives of serotonin: potent agonists for 5-HT1D receptors

Design, Synthesis, and Biological Activity of Novel, Potent, and Selective (Benzoylaminomethyl)thiophene Sulfonamide Inhibitors of c-Jun-N-Terminal Kinase

GLEPP1/Protein-tyrosine Phosphatase ϕ Inhibitors Block Chemotaxis in Vitro and in Vivo and Improve Murine Ulcerative Colitis

G-protein coupled receptors bivalent ligands and drug design

Phosphonate derivatives of N9-benzylguanine: a new class of potent purine nucleoside phosphorylase inhibitors

Studies on the synthesis of the antitumor agent CC-1065. Synthesis of PDE I and PDE II, inhibitors of cyclic adenosine-3',5'-monophosphate phosphodiesterase using the 3,3'-bipyrrole strategy

Discovery and Development of a New Class of Potent, Selective, Orally Active Oxytocin Receptor Antagonists

GLEPP1/Protein-tyrosine Phosphatase φ Inhibitors Block Chemotaxis in Vitro and in Vivo and Improve Murine Ulcerative ColitisS

GLEPP1/Protein-tyrosine Phosphatase Ï Inhibitors Block Chemotaxis in Vitro and in Vivo and Improve Murine Ulcerative Colitis

GLEPP1/Protein-tyrosine Phosphatase {phi} Inhibitors Block Chemotaxis in Vitro and in Vivo and Improve Murine Ulcerative Colitis

Serotonin dimers: application of the bivalent ligand approach to the design of new potent and selective 5-HT(1B/1D) agonists

Serotonin Dimers: Application of the Bivalent Ligand Approach to the Design of New Potent and Selective 5-HT1B/1D Agonists

Differentiation between Partial Agonists and Neutral 5-HT1B Antagonists by Chemical Modulation of 3-[3-(N,N-Dimethylamino)propyl]-4-hydroxy- N-[4-(pyridin-4-yl)phenyl]benzamide (GR-55562)

Section Review: Cardiovascular & Renal: Squalene epoxidase inhibitors

Dimerization of sumatriptan as an efficient way to design a potent, centrally and orally active 5-HT1B agonist

F 11356, a novel 5-hydroxytryptamine (5-HT) derivative with potent, selective, and unique high intrinsic activity at 5-HT1B/1D receptors in models relevant to migraine

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