200 articles for thisTarget
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Article Title
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A series of thiazole derivatives bearing thiazolidin-4-one as non-competitive ADAMTS-5 (aggrecanase-2) inhibitors.
Asahi Kasei Pharma
Synthesis of derivatives of methyl rosmarinate and their inhibitory activities against matrix metalloproteinase-1 (MMP-1).
Second Military Medical University
Synthesis and preliminary evaluation in tumor bearing mice of new (18)F-labeled arylsulfone matrix metalloproteinase inhibitors as tracers for positron emission tomography.
Universit£
Matrix metalloproteinases (MMPs): chemical-biological functions and (Q)SARs.
Pomona College
Three-dimensional quantitative structure-activity relationship (3D-QSAR) models for a novel class of piperazine-based stromelysin-1 (MMP-3) inhibitors: applying a"divide and conquer" strategy.
University Of Missouri St. Louis
Natural products as a gold mine for selective matrix metalloproteinases inhibitors.
East China University Of Science And Technology
Discovery and evaluation of a non-Zn chelating, selective matrix metalloproteinase 13 (MMP-13) inhibitor for potential intra-articular treatment of osteoarthritis.
Alantos Pharmaceuticals
Antidotes to anthrax lethal factor intoxication. Part 3: Evaluation of core structures and further modifications to the C2-side chain.
Panthera Biopharma
Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.
University Of Florida
Discovery of novel selective HER-2 sheddase inhibitors through optimization of P1 moiety.
Incyte
1-Hydroxy-2-pyridinone-based MMP inhibitors: synthesis and biological evaluation for the treatment of ischemic stroke.
Johnson & Johnson Pharmaceutical Research And Development
Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.
Johnson & Johnson Pharmaceutical Research & Development
Syntheses and in vitro evaluation of arylsulfone-based MMP inhibitors with heterocycle-derived zinc-binding groups (ZBGs).
Johnson & Johnson Pharmaceutical Research And Development
Noreupenifeldin, a tropolone from an unidentified ascomycete.
Merck Research Laboratories
Carbamoylphosphonate matrix metalloproteinase inhibitors 6: cis-2-aminocyclohexylcarbamoylphosphonic acid, a novel orally active antimetastatic matrix metalloproteinase-2 selective inhibitor--synthesis and pharmacodynamic and pharmacokinetic analysis.
The Hebrew University Of Jerusalem
Quinazolinones and pyrido[3,4-d]pyrimidin-4-ones as orally active and specific matrix metalloproteinase-13 inhibitors for the treatment of osteoarthritis.
Pfizer
Alpha,beta-cyclic-beta-benzamido hydroxamic acids: novel templates for the design, synthesis, and evaluation of selective inhibitors of TNF-alpha converting enzyme (TACE).
Bristol-Myers Squibb Research And Development
N-i-Propoxy-N-biphenylsulfonylaminobutylhydroxamic acids as potent and selective inhibitors of MMP-2 and MT1-MMP.
Universit£
Carbamoylphosphonates, a new class of in vivo active matrix metalloproteinase inhibitors. 1. Alkyl- and cycloalkylcarbamoylphosphonic acids.
The Hebrew University Of Jerusalem
Stereospecific synthesis of 5-substituted 2-bisarylthiocyclopentane carboxylic acids as specific matrix metalloproteinase inhibitors.
Institut De Recherches Servier
Synthesis and structure-activity relationship of N-substituted 4-arylsulfonylpiperidine-4-hydroxamic acids as novel, orally active matrix metalloproteinase inhibitors for the treatment of osteoarthritis.
Wyeth Research
New type of metalloproteinase inhibitor: design and synthesis of new phosphonamide-based hydroxamic acids.
Nippon Organon K.K.
Design, synthesis, and structure-activity relationships of macrocyclic hydroxamic acids that inhibit tumor necrosis factor alpha release in vitro and in vivo.
Dupont Pharmaceuticals
Potent and selective carboxylic acid-based inhibitors of matrix metalloproteinases.
TBA
Structure-activity relationships and pharmacokinetic analysis for a series of potent, systemically available biphenylsulfonamide matrix metalloproteinase inhibitors.
Parke-Davis Pharmaceutical Research
Design, synthesis, and biological evaluation of potent thiazine- and thiazepine-based matrix metalloproteinase inhibitors.
Procter And Gamble Pharmaceuticals
Design and synthesis of phosphinamide-based hydroxamic acids as inhibitors of matrix metalloproteinases.
Procter And Gamble Pharmaceuticals
Discovery of potent, achiral matrix metalloproteinase inhibitors.
Procter And Gamble Pharmaceuticals
Pyran-containing sulfonamide hydroxamic acids: potent MMP inhibitors that spare MMP-1.
Pfizer
Heterocycle-based MMP inhibitors with P2' substituents.
Procter And Gamble Pharmaceuticals
Arylsulphonyl hydroxamic acids: potent and selective matrix metalloproteinase inhibitors.
Celltech-Chiroscience
Macrocyclic hydroxamate inhibitors of matrix metalloproteinases and TNF-alpha production.
Dupont Pharmaceuticals
Synthesis of an array of potential matrix metalloproteinase inhibitors using a sequence of polymer-supported reagents.
University Of Cambridge
Picking the S1, S1' and S2' pockets of matrix metalloproteinases. A niche for potent acyclic sulfonamide inhibitors.
Universit£
In silico scaffold evaluation and solid phase approach to identify new gelatinase inhibitors.
Colosseum Combinatorial Chemistry Centre For Technology (C4T Scarl)
Lead optimisation of selective non-zinc binding inhibitors of MMP13. Part 2.
Astrazeneca
Fragment-based discovery of indole inhibitors of matrix metalloproteinase-13.
Boehringer Ingelheim Pharmaceuticals
Novel 1-hydroxypiperazine-2,6-diones as new leads in the inhibition of metalloproteinases.
Instituto Superior T£Cnico
Discovery of potent and selective matrix metalloprotease 12 inhibitors for the potential treatment of chronic obstructive pulmonary disease (COPD).
Pfizer
Identification of novel molecular scaffolds for the design of MMP-13 inhibitors: a first round of lead optimization.
Universit£
Discovery of novel Cobactin-T based matrix metalloproteinase inhibitors via a ring closing metathesis strategy.
Johnson & Johnson Pharmaceutical Research & Development
Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes.
University Of Illinois At Chicago
Orally active MMP-1 sparinga-tetrahydropyranyl anda-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
Pfizer
Synthesis and biological evaluation in U87MG glioma cells of (ethynylthiophene)sulfonamido-based hydroxamates as matrix metalloproteinase inhibitors.
Universit£
Structure and activity relationships of tartrate-based TACE inhibitors.
Merck Research Laboratories
MMP-13 selectivea-sulfone hydroxamates: a survey of P1' heterocyclic amide isosteres.
Pfizer
2-(2-Aminothiazol-4-yl)pyrrolidine-based tartrate diamides as potent, selective and orally bioavailable TACE inhibitors.
Merck Research Laboratories
Discovery of (1S,2R,3R)-2,3-dimethyl-2-phenyl-1-sulfamidocyclopropanecarboxylates: novel and highly selective aggrecanase inhibitors.
Central Pharmaceutical Research Institute
Structure based optimization of chromen-based TNF-a converting enzyme (TACE) inhibitors on S1' pocket and their quantitative structure-activity relationship (QSAR) study.
Yonsei University
Novel TNF-a converting enzyme (TACE) inhibitors as potential treatment for inflammatory diseases.
Merck Research Laboratories
Orally bioavailable dual MMP-1/MMP-14 sparing, MMP-13 selective alpha-sulfone hydroxamates.
Pfizer
The discovery of novel tartrate-based TNF-alpha converting enzyme (TACE) inhibitors.
Schering-Plough Research Institute
Discovery of (pyridin-4-yl)-2H-tetrazole as a novel scaffold to identify highly selective matrix metalloproteinase-13 inhibitors for the treatment of osteoarthritis.
Pfizer
The identification of beta-hydroxy carboxylic acids as selective MMP-12 inhibitors.
Gsk Medicines Research Centre
Design, synthesis, biological evaluation, and NMR studies of a new series of arylsulfones as selective and potent matrix metalloproteinase-12 inhibitors.
Universit£
Identification of an orally efficacious matrix metalloprotease 12 inhibitor for potential treatment of asthma.
Wyeth Research
N-O-isopropyl sulfonamido-based hydroxamates: design, synthesis and biological evaluation of selective matrix metalloproteinase-13 inhibitors as potential therapeutic agents for osteoarthritis.
Universit£
Discovery of novel hydroxamates as highly potent tumor necrosis factor-alpha converting enzyme inhibitors. Part II: optimization of the S3' pocket.
Schering-Plough Research Institute
Mercaptoacyl matrix metalloproteinase inhibitors: The effect of substitution at the mercaptoacyl moiety
TBA
Potent carboxylate inhibitors of stromelysin containing P2′ piperazic acids and P1′ biaryl moeities
TBA
Potent matrix metalloproteinase inhibitors: Amino-carboxylate compounds containing modifications of the P1 residue
TBA
Design, synthesis, activity, and structure of a novel class of matrix metalloproteinase inhibitors containing a heterocyclic P2′-P3′ amide bond isostere
TBA
Inhibition of matrix metalloproteinases by N-carboxyalkyl peptides containing extended alkyl residues At P1'
TBA
Hydroxamate inhibitors of the matrix metallo-proteinases (MMPs) containing novel P1′ heteroatom based modifications
TBA
Inhibition of matrix metalloproteinases by N-carboxyalkyl dipeptides: Enhanced potency and selectivity with substituted P1′ homophenylalanines
TBA
Potent and selective inhibitors of gelatinase-A 2. carboxylic and phosphonic acid derivatives
TBA
Compelling P1 substituent affect on metalloprotease binding profile enables the design of a novel cyclohexyl core scaffold with excellent MMP selectivity and HER-2 sheddase inhibition.
Incyte
Synthesis of hydroxypyrone- and hydroxythiopyrone-based matrix metalloproteinase inhibitors: developing a structure-activity relationship.
University Of California
Succinyl hydroxamates as potent and selective non-peptidic inhibitors of procollagen C-proteinase: design, synthesis, and evaluation as topically applied, dermal anti-scarring agents.
Pfizer
Specific targeting of metzincin family members with small-molecule inhibitors: progress toward a multifarious challenge.
University Of Athens
Introduction of the 4-(4-bromophenyl)benzenesulfonyl group to hydrazide analogs of Ilomastat leads to potent gelatinase B (MMP-9) inhibitors with improved selectivity.
Université
The berkeleyamides, amides from the acid lake fungus Penicillum rubrum.
Montana Tech Of The University Of Montana
Pharmacologic inhibition of tpl2 blocks inflammatory responses in primary human monocytes, synoviocytes, and blood.
Wyeth Research
Peptidyl 3-substituted 1-hydroxyureas as isosteric analogues of succinylhydroxamate MMP inhibitors.
Università
Discovery and characterization of a novel inhibitor of matrix metalloprotease-13 that reduces cartilage damage in vivo without joint fibroplasia side effects.
Pfizer
beta-N-Biaryl ether sulfonamide hydroxamates as potent gelatinase inhibitors: part 2. Optimization of alpha-amino substituents.
Johnson & Johnson Pharmaceutical Research And Development
Conversion of an MMP-potent scaffold to an MMP-selective HER-2 sheddase inhibitor via scaffold hybridization and subtle P1' permutations.
Incyte
Design and identification of selective HER-2 sheddase inhibitors via P1' manipulation and unconventional P2' perturbations to induce a molecular metamorphosis.
Incyte
Platinum complexes can inhibit matrix metalloproteinase activity: platinum-diethyl[(methylsulfinyl)methyl]phosphonate complexes as inhibitors of matrix metalloproteinases 2, 3, 9, and 12.
Università
Synthesis and structure-activity relationship of a novel, non-hydroxamate series of TNF-alpha converting enzyme inhibitors.
Bristol-Myers Squibb Pharmaceutical Research Institute
Simultaneous presence of unsaturation and long alkyl chain at P'1 of Ilomastat confers selectivity for gelatinase A (MMP-2) over gelatinase B (MMP-9) inhibition as shown by molecular modelling studies.
Université
Hydantoins, triazolones, and imidazolones as selective non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).
Bristol-Myers Squibb Pharmaceutical Research Institute
A new 4-(2-methylquinolin-4-ylmethyl)phenyl P1' group for the beta-amino hydroxamic acid derived TACE inhibitors.
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and in vitro evaluation of targeted tetracycline derivatives: effects on inhibition of matrix metalloproteinases.
Clermont Auvergne University
Discovery of a potent, selective, and orally active human epidermal growth factor receptor-2 sheddase inhibitor for the treatment of cancer.
Incyte
alpha-Biphenylsulfonylamino 2-methylpropyl phosphonates: enantioselective synthesis and selective inhibition of MMPs.
Università
Identification of potent and selective TACE inhibitors via the S1 pocket.
Wyeth Research
Discovery of low nanomolar non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and SAR of alpha-sulfonylcarboxylic acids as potent matrix metalloproteinase inhibitors.
Johnson & Johnson Pharmaceutical Research And Development
A cassette-dosing approach for improvement of oral bioavailability of dual TACE/MMP inhibitors.
Novartis Institutes For Biomedical Research
Synthesis and structure-activity relationship of a novel, achiral series of TNF-alpha converting enzyme inhibitors.
Bristol-Myers Squibb Pharmaceutical Research Institute
Matrix metalloproteinase target family landscape: a chemometrical approach to ligand selectivity based on protein binding site analysis.
Aventis Pharma Deutschland
N-Hydroxyurea as zinc binding group in matrix metalloproteinase inhibition: mode of binding in a complex with MMP-8.
Università
Structure-based design and synthesis of novel non-zinc chelating MMP-12 inhibitors.
Pfizer
Discovery of 3-OH-3-methylpipecolic hydroxamates: potent orally active inhibitors of aggrecanase and MMP-13.
Pfizer
QSAR-by-NMR: quantitative insights into structural determinants for binding affinity by analysis of 1H/15N chemical shift differences in MMP-3 ligands.
Aventis Pharma Deutschland
Structure-based design of potent and selective inhibitors of collagenase-3 (MMP-13).
Pharmaceutical Research Institute
3-Hydroxy-4-arylsulfonyltetrahydropyranyl-3-hydroxamic acids are novel inhibitors of MMP-13 and aggrecanase.
Pfizer
A molecular basis for the selectivity of thiadiazole urea inhibitors with stromelysin-1 and gelatinase-A from generalized born molecular dynamics simulations.
University Of California San Francisco
Azasugar-based MMP/ADAM inhibitors as antipsoriatic agents.
Hokkaido Collaboration Center N-21
Synthesis and biological activity of selective azasugar-based TACE inhibitors.
Organon K.K.
MMPs inhibitors: new succinylhydroxamates with selective inhibition of MMP-2 over MMP-3.
Umr/Cnrs 6013
A potent, selective inhibitor of matrix metalloproteinase-3 for the topical treatment of chronic dermal ulcers.
Pfizer
Design, synthesis and evaluation of novel azasugar-based MMP/ADAM inhibitors.
Hokkaido Collaboration Center
Structure--activity relationships of azasugar-based MMP/ADAM inhibitors.
Hokkaido Collaboration Center
Synthesis of radiolabeled biphenylsulfonamide matrix metalloproteinase inhibitors as new potential PET cancer imaging agents.
Indiana University School Of Medicine
Discovery of selective phosphonamide-based inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).
Organon K.K.
NMR-based modification of matrix metalloproteinase inhibitors with improved bioavailability.
Abbott Laboratories
Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships.
Bristol-Myers Squibb
Encounter with unexpected collagenase-1 selective inhibitor: switchover of inhibitor binding pocket induced by fluorine atom.
Organon K.K.
New strategy for antedrug application: development of metalloproteinase inhibitors as antipsoriatic drugs.
Organon K.K.
Phenoxyphenyl sulfone N-formylhydroxylamines (retrohydroxamates) as potent, selective, orally bioavailable matrix metalloproteinase inhibitors.
Abbott Laboratories
Design of selective and soluble inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).
Glaxosmithkline
Discovery of macrocyclic hydroxamic acids containing biphenylmethyl derivatives at P1', a series of selective TNF-alpha converting enzyme inhibitors with potent cellular activity in the inhibition of TNF-alpha release.
Dupont Pharmaceuticals
Asymmetric synthesis of BB-3497--a potent peptide deformylase inhibitor.
British Biotech Pharmaceuticals
Design and synthesis of matrix metalloproteinase inhibitors guided by molecular modeling. Picking the S(1) pocket using conformationally constrained inhibitors.
Université
N-Aryl sulfonyl homocysteine hydroxamate inhibitors of matrix metalloproteinases: further probing of the S(1), S(1)', and S(2)' pockets.
Université
N-hydroxyformamide peptidomimetics as TACE/matrix metalloprotease inhibitors: oral activity via P1' isobutyl substitution.
Glaxosmithkline
The development of new carboxylic acid-based MMP inhibitors derived from a cyclohexylglycine scaffold.
Procter And Gamble Pharmaceuticals
A new concept for multidimensional selection of ligand conformations (MultiSelect) and multidimensional scoring (MultiScore) of protein-ligand binding affinities.
The Royal Danish School Of Pharmacy
Discovery and characterization of the potent, selective and orally bioavailable MMP inhibitor ABT-770.
Abbott Laboratories
Biaryl ether retrohydroxamates as potent, long-lived, orally bioavailable MMP inhibitors.
Abbott Laboratories
Design and synthesis of 2-oxo-imidazolidine-4-carboxylic acid hydroxyamides as potent matrix metalloproteinase-13 inhibitors.
Pfizer
Novel 5,5-disubstitutedpyrimidine-2,4,6-triones as selective MMP inhibitors.
Roche Research Center
Development of new carboxylic acid-based MMP inhibitors derived from functionalized propargylglycines.
Procter And Gamble Pharmaceuticals
Chemoenzymatic synthesis of functionalized cyclohexylglycines and alpha-methylcyclohexylglycines via Kazmaier-Claisen rearrangement.
University Of Florida
Discovery of potent and selective succinyl hydroxamate inhibitors of matrix metalloprotease-3 (stromelysin-1).
Pfizer
Selectivity of inhibition of matrix metalloproteases MMP-3 and MMP-2 by succinyl hydroxamates and their carboxylic acid analogues is dependent on P3' group chirality.
Pfizer
General synthesis of alpha-substituted 3-bisaryloxy propionic acid derivatives as specific MMP inhibitors.
Institut De Recherches Servier
Development of new hydroxamate matrix metalloproteinase inhibitors derived from functionalized 4-aminoprolines.
Procter And Gamble Pharmaceuticals
Structure-based design and synthesis of a potent matrix metalloproteinase-13 inhibitor based on a pyrrolidinone scaffold.
Pfizer
Design and synthesis of piperazine-based matrix metalloproteinase inhibitors.
Procter And Gamble Pharmaceuticals
Design, synthesis, and biological evaluation of matrix metalloproteinase inhibitors derived from a modified proline scaffold.
University Of Florida
Affinity and selectivity of matrix metalloproteinase inhibitors: a chemometrical study from the perspective of ligands and proteins.
Hoechst Marion Roussel
Selective inhibition of low affinity IgE receptor (CD23) processing: P1' bicyclomethyl substituents.
Smithkline Beecham Pharmaceuticals
The synthesis and biological evaluation of non-peptidic matrix metalloproteinase inhibitors.
British Biotech Pharmaceuticals
P1, P2'-linked macrocyclic amine derivatives as matrix metalloproteinase inhibitors.
Dupont Pharmaceuticals
Discovery of a novel series of selective MMP inhibitors: identification of the gamma-sulfone-thiols.
Searle Discovery Research
Synthesis of a series of stromelysin-selective thiadiazole urea matrix metalloproteinase inhibitors.
Pharmacia And Upjohn
Dual inhibition of phosphodiesterase 4 and matrix metalloproteinases by an (arylsulfonyl)hydroxamic acid template.
RhôNe-Poulenc Rorer
Inhibition of MMP-1 and MMP-13 with phosphinic acids that exploit binding in the S2 pocket.
Pfizer
Aryl ketones as novel replacements for the C-terminal amide bond of succinyl hydroxamate MMP inhibitors.
Abbott Laboratories
The design, synthesis, and structure-activity relationships of a series of macrocyclic MMP inhibitors.
Abbott Laboratories
Design and synthesis of conformationally-constrained MMP inhibitors.
Procter And Gamble Pharmaceuticals
Broad spectrum matrix metalloproteinase inhibitors: an examination of succinamide hydroxamate inhibitors with P1 C alpha gem-disubstitution.
Abbott Laboratories
The asymmetric synthesis and in vitro characterization of succinyl mercaptoalcohol and mercaptoketone inhibitors of matrix metalloproteinases.
Wyeth-Ayerst Research
Malonyl alpha-mercaptoketones and alpha-mercaptoalcohols, a new class of matrix metalloproteinase inhibitors.
Affymax Research Institute
Structure-based design and synthesis of a series of hydroxamic acids with a quaternary-hydroxy group in P1 as inhibitors of matrix metalloproteinases.
Dupont Pharmaceuticals
Rational design and combinatorial evaluation of enzyme inhibitor scaffolds: identification of novel inhibitors of matrix metalloproteinases.
Affymax Research Institute
Design and synthesis of cyclic inhibitors of matrix metalloproteinases and TNF-alpha production.
Dupont Pharmaceuticals
Inhibition of membrane-type 1 matrix metalloproteinase by hydroxamate inhibitors: an examination of the subsite pocket.
Kanebo
Highly selective and orally active inhibitors of type IV collagenase (MMP-9 and MMP-2): N-sulfonylamino acid derivatives.
Shionogi
Dual inhibition of human leukocyte elastase and lipid peroxidation: in vitro and in vivo activities of azabicyclo[2.2.2]octane and perhydroindole derivatives.
Institut De Recherche Servier
Inhibition of stromelysin-1 (MMP-3) by P1'-biphenylylethyl carboxyalkyl dipeptides.
Merck Research Laboratories
A recombinant human stromelysin catalytic domain identifying tryptophan derivatives as human stromelysin inhibitors.
Warner-Lambert
Inhibition of matrix metalloproteinases by N-carboxyalkyl peptides.
Merck Research Laboratories
Matrix metalloproteinase inhibitors containing a (carboxyalkyl)amino zinc ligand: modification of the P1 and P2' residues.
Glaxo Inc. Research Institute
Inhibition of matrix metalloproteinases by hydroxamates containing heteroatom-based modifications of the P1' group.
Sterling Winthrop Pharmaceuticals Research Division
In vitro binding characteristics of a new selective group II metabotropic glutamate receptor radioligand, [3H]LY354740, in rat brain.
F. Hoffmann-La Roche
Novel flufenamic acid analogues as inhibitors of androgen receptor mediated transcription.
St. Jude Research Hospital
Scaffold hopping, synthesis and structure-activity relationships of 5,6-diaryl-pyrazine-2-amide derivatives: a novel series of CB1 receptor antagonists.
Astrazeneca
Discovery of a series of acrylic acids and their derivatives as chemical leads for selective EP3 receptor antagonists.
Ono Pharmaceutical
Antagonists of the human A(2A) receptor. Part 6: Further optimization of pyrimidine-4-carboxamides.
Vernalis (R&D)